CAS: 86-48-6; 1-Hydroxy-2-Naphthoic Acid

该化合物是一种氯化萘衍生物,分别具有1个和2个位置的氢氧基和箱酸功能组,该化合物是有机合成的多用途中间体,特别是在染料,颜料和药品生产方面,其双功能结构允许选择性反应,允许在混合反应,协调化学和复杂乙型循环合成中应用.该化合物在极地有机溶剂中表现出中等溶性,便于其在溶液阶段反应中使用.在标准条件下其稳定性和特征清晰的再活性简介使它成为精细化学和材料科学应用研究人员的可靠建筑块.

英文名称1-Hydroxy-2-Naphthoic Acid
中文名称1-羟基-2-萘甲酸
IUPAC名称1-hydroxy-2-naphthoic acid
其它别名Inchi=1/c11H8O3/c12-10-8-4-2-1-3-7(8)5-6-9(10)11(13)14/h1-6,12H,(H,13,14; 7-Naphthol-2-Carboxaldehyde; Carboxynaphthol; 1-Hydroxy-2-Naphthalene Carboxylic Acid; En30
CAS编号86-48-6
MFCD编号:MFCD00003960
EINECS号:201-674-0
FDA UNII编号:U8LZ3R07L8
分子式:C11H8O3
分子量:188.18
产品CID: 1867078
产品分类有机原料 → 羧酸类化合物及衍生物 → 羧酸的卤化、磺化、硝化或亚硝化衍生物

相似结构搜索
InChIKey: SJJCQDRGABAVBB-UHFFFAOYSA-N
InChI=1S/C11H8O3/c12-10-8-4-2-1-3-7(8)5-6-9(10)11(13)14/h1-6,12H,(H,13,14)…
计算化学: 氢键受体数3.0氢键供体数2.0可旋转键数1.0

物理性质

熔点195-200 °C (分解)(文献)
沸点367.7±25.0 °C at 760 mmHg
闪点190.4±19.7 °C
密度1.4±0.1 g/cm3
pKa:3.02±0.30(预测)
PSA:57.53
LogP:3.29
折射率1.716
蒸汽压0.0±0.9 mmHg at 25°C
溶解性Alcohol: Freely Soluble
敏感性本品有毒。其生理作用与羟基羧酸相似。生产本品所使用的溶剂氯苯具有麻醉性，能刺激皮肤；盐酸为挥发性气体，刺激皮肤及黏膜，容易引起咽炎。生产过程中应加强劳动保护，操作人员应穿戴好劳动保护用具。
外观形态白色至微粉红色至棕褐色粉末或晶体
储存条件密封, 常温干燥保存
产品应用该品为染料和彩色胶片成色剂的中间体,也用于其他有机合成和用作电池添加剂.
性质描述白色至微红色结晶.熔点191-192°C,溶于乙醇,乙醚,苯,三氯甲烷和碱性溶液中,微溶于热水,几乎不溶于冷水.

MSDS等安全信息

GHS象形图
GHS符号GHS07;
注释: Exclamation mark
危险类别特定目标器官毒性 - 单次接触类别3
皮肤腐蚀/刺激类别2
严重眼刺激类别2
严重眼刺激类别2A
急性毒性类别4(经口)
严重眼损伤类别1
警示词Warning(警告)
危险描述H335 |可能引起呼吸道刺激.
H315 |造成皮肤刺激.
H319 |造成严重眼刺激.
H302 |吞咽有害.
H318 |造成严重眼损伤.
防范说明P261-P264-P271-P280-P302+P352-P305+P351+P338
UN编号NONH for all modes of transport
危险品标志Xi
安全声明26-36-37/39-37
危险类别码36/37/38
WGK Germany3

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

合成工艺路线路线简述

合成目标产物 1-Hydroxy-2-Naphthoic Acid 主要起始原料 1-Naphthol
89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Acetone; 3 - 4 H,25 - 35 °C
标题:Preparation Of Salmeterol And Salts Thereof
参考文献:India]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Methanol; 1 H,30 °C; 30 °C -> 22 °C; 2 H,18 - 22 °C
标题:Improved Process For The Preparation Of Salmeterol Xinafoate
参考文献:India]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Isopropanol; Rt -> 70 °C; 8 H,70 °C
标题:Synthesis Route Of Salmeterol Xinafoate
作者:Jiang,Zhi-Gan; Hua,Zheng-Mao; Mai,Lu-Gen; Yang,Li-Ge
参考文献:Huadong Shifan Daxue Xuebao 日期:2003 卷标:(3) 页码:102-104]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Preparation Of Salmeterol And Its Application
参考文献:China]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Utility Of Von Pechman Synthesis Of Coumarin Reaction For Development Of Spectrofluorimetric Method For Quantitation Of Salmeterol Xinafoate In Pharmaceutical Preparations And Human Plasma
作者:Awad,Mohamed; Hammad,Mohamed A.; Abdel-Megied,Ahmed M.; Omar,Mahmoud A.
参考文献:Luminescence 日期:2018 卷标:33(5) 页码:913-918]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Improved Process For The Preparation A Long-Acting β2-Adrenergic Agonist (Laba) Salmeterol And Identification,Characterization And Control Of Its Potential Process Impurity
作者:Reddy,Sahadeva; Rajan,S. T.; Parusuramudu; Reddy,Raghupathi; Chakravarthy,I. E.
参考文献:Pharma Chemica 日期:2016 卷标:8(8) 页码:28-35]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Process For Preparation Of Salmeterol
参考文献:India]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:An Improved Process For The Preparation Of Salmeterol Xinafoate
参考文献:India]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Phenethanolamine Derivatives Useful In The Treatment Of Respiratory Problems
参考文献:Federal Republic Of Germany]

574-96-9 = 86-48-6
反应条件:1.1 Reagents: Oxygen Solvents: Water; Rt -> 37 °C; 24 H,Ph 7,1 Atm,37 °C
标题:Catalyst-Free Aerobic Oxidation Of Aldehydes Into Acids In Water Under Mild Conditions
作者:Zhang,Yue; Et Al
参考文献:Green Chemistry 日期:2017 卷标:19(23) 页码:5708-5713]

17201-44-4 + 90-15-3 = 86-48-6
反应条件:1.1 4 H,1.2 - 1.4 Atm,Rt -> 160 °C; 1 H,160 °C1.2 Reagents: Hydrochloric Acid Solvents: Water
标题:Carboxylation Of Naphthols With Sodium Ethyl Carbonate
作者:Suerbaev,Kh. A.; Et Al
参考文献:Neftekhimiya 日期:2005 卷标:45(5) 页码:364-366]

17201-44-4 + 90-15-3 = 86-48-6
反应条件:1.1 Reagents: Oxygen; 1 H,Rt -> 60 °C; 4 H,1.2 - 1.4 Atm,60 °C -> 160 °C; 1 H,160 °C; 160 °C -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Rt
标题:Carboxylation Of Hydroxyarenes With Metal Alkyl Carbonates
作者:Suerbaev,Khakim A.; Et Al
参考文献:Green Processing And Synthesis 日期:2015 卷标:4(2) 页码:91-96]

121453-00-7 + 86-48-6 = 86-48-6
反应条件:1.1 Reagents: Triethylamine,Iron Perchlorate Hexahydrate Solvents: Methanol; Rt; 4 H,Rt
标题:Mimicking The Aromatic-Ring-Cleavage Activity Of Gentisate-1,2-Dioxygenase By A Nonheme Iron Complex
作者:Rahaman,Rubina; Et Al
参考文献:Angewandte Chemie 日期:2016 卷标:55(44) 页码:13838-13842]

1344113-50-3 = 86-48-6
反应条件:1.1 Reagents: 2,2,2-Trifluoroethanol,Silver Acetate Catalysts: Palladium Diacetate,Boc-L-Leucine Solvents: 1,2-Dichloroethane; 5 Min,95 °C; 18 H,95 °C1.2 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 30 Min,Rt
标题:General Method For The Synthesis Of Salicylic Acids From Phenols Through Palladium-Catalyzed Silanol-Directed C-H Carboxylation
作者:Wang,Yang; Et Al
参考文献:Angewandte Chemie 日期:2015 卷标:54(7) 页码:2255-2259]

90-15-3 = 86-48-6
反应条件:1.1 Reagents: Ethyl Bromide,Magnesium Solvents: Diethyl Ether1.2 Solvents: Carbon Disulfide1.3 Reagents: Ammonium Chloride Solvents: Water
标题:Metal Template Ortho-Acylation Of Phenols. Direct Synthesis Of Salicylic Acid Chlorides And Derivatives
作者:Sartori,Giovanni; Et Al
参考文献:Synthesis 日期:1988 卷标:(10) 页码:763-6]

= 86-48-6
反应条件:1.1 Solvents: Carbon Disulfide1.2 Reagents: Ammonium Chloride Solvents: Water
标题:Metal Template Ortho-Acylation Of Phenols. Direct Synthesis Of Salicylic Acid Chlorides And Derivatives
作者:Sartori,Giovanni; Et Al
参考文献:Synthesis 日期:1988 卷标:(10) 页码:763-6]

7732-44-7 = 86-48-6
反应条件:1.1 Catalysts: Ethyl Acetoacetate
标题:Studies On 1-Hydroxy-2-Naphthoic And 3-Hydroxy-2-Naphthoic Acid Hydrazides
作者:Pant,U. C.; Et Al
参考文献:Revue Roumaine De Chimie 日期:1979 卷标:24(3) 页码:471-82]

90-15-3 = 86-48-6
反应条件:1.1 Reagents: Triethylaluminum Solvents: Diethyl Ether,Hexane2.1 Solvents: Carbon Disulfide2.2 Reagents: Ammonium Chloride Solvents: Water
标题:Metal Template Ortho-Acylation Of Phenols. Direct Synthesis Of Salicylic Acid Chlorides And Derivatives
作者:Sartori,Giovanni; Et Al
参考文献:Synthesis 日期:1988 卷标:(10) 页码:763-6]

= 86-48-6
反应条件:1.1 -2.1 Reagents: Oxygen; 1 H,Rt -> 60 °C; 4 H,1.2 - 1.4 Atm,60 °C -> 160 °C; 1 H,160 °C; 160 °C -> Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Rt
标题:Carboxylation Of Hydroxyarenes With Metal Alkyl Carbonates
作者:Suerbaev,Khakim A.; Et Al
参考文献:Green Processing And Synthesis 日期:2015 卷标:4(2) 页码:91-96]

80317-59-5 + 3401-47-6 = 86-48-6
反应条件:1.1 Reagents: Magnesium,Dibromoethane Solvents: Diethyl Ether,Benzene; Heated; Overnight,Reflux1.2 Solvents: Benzene; 1 H,Reflux1.3 Reagents: Ammonium Chloride Solvents: Water2.1 Reagents: Hydrochloric Acid Solvents: Water; 36 H,Reflux
标题:Synthesis Of Chiral Binaphthyl Derivatives
作者:Wilson,Janet M.
参考文献:1981]

= 86-48-6
反应条件:1.1 Reagents: Magnesium,Iodine,Dibromoethane,2-(1-Bromo-2-Naphthalenyl)-4,5-Dihydro-4,4-Dimethyloxazole Solvents: Diethyl Ether; 5 H,Reflux1.2 Solvents: Tetrahydrofuran; 13 H,Reflux1.3 Reagents: Ammonium Chloride Solvents: Water2.1 Reagents: Hydrochloric Acid Solvents: Water; 36 H,Reflux
标题:Synthesis Of Chiral Binaphthyl Derivatives
作者:Wilson,Janet M.
参考文献:1981]

93530-92-8 + 101143-87-7 = 86-48-6
反应条件:1.1 Reagents: Sodium Hydride Solvents: Dimethylformamide; 4 H,Rt; Rt -> 60 °C; 24 H,60 °C1.2 18 H,56 °C1.3 Reagents: Ammonium Chloride Solvents: Water; Neutralized1.4 Reagents: Hydrochloric Acid Solvents: Water2.1 Reagents: Magnesium,Dibromoethane Solvents: Diethyl Ether,Benzene; Overnight,Reflux2.2 Solvents: Benzene; 45 Min,Reflux; Reflux -> Rt2.3 Reagents: Ammonium Chloride Solvents: Water3.1 Reagents: Hydrochloric Acid Solvents: Water; 36 H,Reflux
标题:Synthesis Of Chiral Binaphthyl Derivatives
作者:Wilson,Janet M.
参考文献:1981]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Methyl Ethyl Ketone; Rt
标题:Process For The Preparation Of Salmeterol Xinafoate From 2-(Bromoethyl)Benzene
参考文献:China]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Acetone; 40 Min,30 °C
标题:Preparation Method Of Salmeterol Xinafoate
参考文献:China]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Acetone; 30 Min,45 °C; 45 °C -> 25 °C; 1 H,25 °C1.2 Solvents: Tert-Butyl Methyl Ether; 25 °C -> 10 °C; 2 H,10 °C
标题:Process For Preparation Of Salmeterol
参考文献:World Intellectual Property Organization]

934842-69-0 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Ethanol; Rt
标题:A New Route For Synthesis Of Salmeterol Xinafoate
作者:Wu,Xiaochun
参考文献:Xinan Shifan Daxue Xuebao 日期:2009 卷标:34(4) 页码:85-88]

262857-01-2 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Reagents: Acetic Acid Solvents: Water; 3 H,70 °C1.2 Solvents: Ethyl Acetate; 16 H,Rt
标题:Preparation Of Deuterium Substituted Ethanolamines As Adrenergic Modulators For Disease Treatment
参考文献:United States]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Methanol; 25 - 30 °C; 3 H,0 °C
标题:A Method For Preparing Salmeterol Hydroxynaphthoate
参考文献:China]

89365-50-4 + 86-48-6 = 86-48-6 + 89365-50-4
反应条件:1.1 Solvents: Methanol,Ethyl Acetate
标题:Preparation Of Salmeterol Xinafolate
作者:Anonymous
参考文献:Research Disclosure 日期:2006 卷标:506]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Process For The Preparation Of Crystalline Salmeterol And Its Xinafoate Salt
参考文献:World Intellectual Property Organization]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Process For Preparation Of Salmeterol Xinafoate
参考文献:World Intellectual Property Organization]

= 86-48-6 + 89365-50-4 [标题:Reaction Conditions
标题:Medicaments Containing Betamimetic Drugs And A Novel Anticholinesterase Drug For Treating Respiratory Tract Diseases
参考文献:World Intellectual Property Organization]

90-15-3 = 86-48-6
反应条件:1.1 Solvents: 3-Methoxybutanol
标题:Process For Preparation Of Aromatic Carboxylic Acids By Carboxylation Of Aromatic Compounds In Alkoxyalkanols As Solvents
参考文献:European Patent Organization]

90-15-3 + 4861-79-4 = 86-48-6
反应条件:1.1 Solvents: Dimethylformamide
标题:An Efficient Carboxylation Of 1-Naphthols Using Magnesium Methyl Carbonate
作者:Cate,Laurence A.
参考文献:Synthesis 日期:1983 卷标:(5) 页码:385-6]

17201-44-4 + 90-15-3 = 86-48-6
反应条件:1.1 4 H,1 Atm -> 1.1 Atm,Rt -> 160 °C; 1 H,1.1 - 1.2 Atm,160 °C; 160 °C -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified,Rt
标题:Carboxylation Of Hydroxy Arenes By Alkaline Metal Salts Of Ethylcarbonic Acid
作者:Shalmagambetov,K. M.; Et Al
参考文献:Khimicheskaya Tekhnologiya (Moscow 日期:2011 卷标:12(10) 页码:598-603]

345621-89-8 = 86-48-6
反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; 36 H,Reflux
标题:Synthesis Of Chiral Binaphthyl Derivatives
作者:Wilson,Janet M.
参考文献:1981]

19402-71-2 = 86-48-6
反应条件:1.1 Solvents: Nitrobenzene
标题:The Carboxylation Of Naphthols By Kolbe-Schmitt Reaction In The Homogeneous Solution
作者:Yamaguchi,Tatsuaki; Et Al
参考文献:Nippon Kagaku Kaishi 日期:1989 卷标:(7) 页码:1164-5]

90-15-3 + 298-14-6 = 86-48-6
反应条件:1.1 Catalysts: Decarboxylase Solvents: Acetonitrile,Water; 24 H,Ph 8.5,30 °C
标题:Regioselective Enzymatic Carboxylation Of Phenols And Hydroxystyrene Derivatives
作者:Wuensch,Christiane; Et Al
参考文献:Organic Letters 日期:2012 卷标:14(8) 页码:1974-1977]

90-15-3 = 86-48-6 [标题:Reaction Conditions
标题:1-Hydroxy-2-Naphthoic Acid
参考文献:Romania]

90-15-3 = 86-48-6
反应条件:1.1 Reagents: Sodium Bicarbonate,Potassium Bicarbonate Solvents: Water
标题:Synthesis Of Menadione
作者:Rao,A. V. Rama; Et Al
参考文献:Indian Journal Of Chemistry 日期:1985 卷标:(3) 页码:233-5]

80373-29-1 + 3401-47-6 = 86-48-6
反应条件:1.1 Reagents: Magnesium,Dibromoethane Solvents: Diethyl Ether,Benzene; Overnight,Reflux1.2 Solvents: Benzene; 45 Min,Reflux; Reflux -> Rt1.3 Reagents: Ammonium Chloride Solvents: Water2.1 Reagents: Hydrochloric Acid Solvents: Water; 36 H,Reflux
标题:Synthesis Of Chiral Binaphthyl Derivatives
作者:Wilson,Janet M.
参考文献:1981]

94403-14-2 + 90-15-3 = 86-48-6
反应条件:1.1 Reagents: Imidazole Solvents: Dimethylformamide; 0 °C; 30 Min,Rt1.2 Solvents: Dimethylformamide; 0 °C; Overnight,Rt2.1 Reagents: 2,2,2-Trifluoroethanol,Silver Acetate Catalysts: Palladium Diacetate,Boc-L-Leucine Solvents: 1,2-Dichloroethane; 5 Min,95 °C; 18 H,95 °C2.2 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 30 Min,Rt
标题:General Method For The Synthesis Of Salicylic Acids From Phenols Through Palladium-Catalyzed Silanol-Directed C-H Carboxylation
作者:Wang,Yang; Et Al
参考文献:Angewandte Chemie 日期:2015 卷标:54(7) 页码:2255-2259

6-Hydroxy-2,3-Benzotropon置于palladium On Activated Charcoal Tetrafluoroboric Acid,水,氢气,Sodium Nitrite体系中,化学反应生成 1-羟基-2-萘甲酸
参考文献:3,4-苯并托酚酮和相关化合物.八.6-Hydroxy-2,3-Benzotropone 的偶氮,硝基和氨基衍生物
标题:3,4-苯并托酚酮和相关化合物.八.6-Hydroxy-2,3-Benzotropone 的偶氮,硝基和氨基衍生物
摘要:在重氮偶联和硝化作用下,6-羟基-2,3-苯并托酮 (I) 及其 5-溴衍生物 (II) 分别得到 7-偶氮(v 和 Vi)和 7-硝基取代产物(vii 和 Viii) . 在相同的反应中,7-溴-6-羟基-(Iii) 和 5,7-二溴-6-羟基-2,3-苯并托酮 (Iv) 取代了它们的 7-溴取代基,得到相同的 7-偶氮和 7-硝基取代产物如上.在 Iii 和 Iv 的硝化作用中,还形成了 2,2-二溴-(Ix) 和 2,2,7-三溴-4,5-苯并环庚-4,6-二烯-1,3-二酮 (X).v,Vi,Vii 和 Viii 的氢化得到 7-Amino-6-Hydroxy-2,3-Benzotropone (Xi),重氮化得到 2-Diazo-4,5-Benzocyclohepta-4,6-Diene-1,3-二酮 (Xii).7-Chloro-6-Hydroxy-2,3-Benzotropone
DOI:10.1246/bcsj.43.1778

海关参考信息

2902902000-精萘
2905110000-甲醇
2906210000-苄醇
2912110000-甲醛
💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
详情请参考：📖 海关编码查询和海关进出口税则

专利信息

专利号:US-10918627-B2
优先权日:2016-05-11
标题:Convergent and enantioselective total synthesis of Communesin analogs
发明人：MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.

专利号:US-3772389-A
优先权日:1971-06-24
标题:Process for the synthesis of phenyl esters
发明人：LOWRANCE W
权利人:EASTMAN KODAK CO
摘要:A PROCESS FOR THE SYNTHESIS OF PHENYL ESTERS DIRECTLY FROM THE CORRESPONDING PHENOLS AND CARBOXYLIC ACIDS WHICH COMPRISES CONTACTING A PHENOLIC COMPOUND HAVING AT LEAST ONE HYDROGEN ATOM ADJACENT THE ACTIVE HYDROXYL GROUP WITH A CARBOXYLIC ACID COMPOUND CONTAINING AT LEAST ONE ACTIVE CARBOXYLIC GROUP IN THE PRESENCE OF A CATALYTIC AMOUNT OF A BORATE-SULFURIC ACID CATALYST COMPLEX. THE PROCESS IS CARRIED OUT IN A SINGLE STAGE REACTOR WHICH MAY BE OPERATED AT FROM 75*C. TO 285*C. UNDER ATMOSPHERIC, SUBATMOSPHERIC OR SUPERATMOSPHERIC PRESSURE. IF DESIRABLE, A SOLVENT CAN BE EMPLOYED.

专利号:WO-2024104433-A9
优先权日:2022-11-16
标题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament
发明人：ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING
权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING
摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.

专利号:US-9981949-B2
优先权日:2008-12-01
标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine
发明人：AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT
权利人:OYSTER POINT PHARMA INC
摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.

专利号:US-8604191-B2
优先权日:2008-12-01
标题:Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3YLVINYL)pyrimidine
发明人：AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT
权利人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; TARGACEPT INC
摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.

专利号:US-9359327-B2
优先权日:2008-06-30
标题:Process for the preparation of substituted pyrimidine derivatives
发明人：CESCO-CANCIAN SERGIO; CHEN HONGFENG; GRIMM JEFFREY S; MANI NEELAKANDHA S; MAPES CHRISTOPHER M; PALMER DAVID C; PIPPEL DANIEL J; SORGI KIRK L; XIAO TONG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H 4 receptor modulators, and to intermediates in H4 modulator synthesis.

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合成参考文献

参考文献:10.1016/j.bmc.2011.06.080
摘要:Liu KC, Lee PS, Wang SY, Cheng YS, Fang JM, Wong CH. Intramolecular ion-pair prodrugs of zanamivir and guanidino-oseltamivir. Bioorg Med Chem. 2011 Aug 15;19(16):4796–802. doi: 10.1016/j.bmc.2011.06.080.