- 英文名称Tert-Butyl 4-(4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1H-Pyrazol-1-yl)Piperidine-1-Carboxylate
- 中文名称4-[4-(4,4,5,5-四甲基-1,3,2-二氧杂环戊硼烷-2-基)-1H-吡唑-1-基]哌啶-1-甲酸叔丁酯
- IUPAC名称tert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
- 其它别名4-[4-(4,4,5,5-四甲基-1,3,2-二氧硼戊环-2-基)吡唑-1-基]哌啶-1-甲酸叔丁酯; Tert-Butyl 4-[4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1H-Pyrazol-1-Yl]Piperidine-1-Carboxylate
- CAS编号877399-74-1
- MFCD编号:MFCD11112131
- EINECS号:800-459-4
- FDA UNII编号:6T7DZ73552
- 分子式:C19H32BN3O4
- 分子量:377.29
- 产品CID: 1886008
- 产品分类有机原料→分子砌块→芳杂环类化合物→吡唑类化合物
相似化合物
1190875-39-8 1323919-64-7 1175273-62-7欧盟法规
ECHA物质C&L通报上下游产品
CAS号877399-73-0 1-B°C-4-(4-碘-1H... | CAS号73183-34-3 双戊酰二硼 | CAS号141699-59-4 1-B°C-4-甲烷磺酰氧基哌啶 | CAS号269410-08-4 4-吡唑硼酸频哪醇酯 | CAS号877399-50-3 4-(4-溴吡唑-1-基)哌啶... | CAS号61676-62-8 2-异丙氧基-4,4,5,5-... | CAS号1195-66-0 2-甲氧基-4,4,5,5-四... | CAS号109384-19-2 N-B°C-4-羟基哌啶 | CAS号5382-16-1 4-羟基哌啶 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1175273-62-7 1-(4-哌啶基)-1H-吡唑...合成工艺路线路线简述
- 877399-50-3 + 61676-62-8 = 877399-74-1
反应条件:1.1 Reagents: Chloro(1-Methylethyl)Magnesium Solvents: Tetrahydrofuran; 12 H,20 - 30 °C1.2 Solvents: Tetrahydrofuran; 6 H,20 - 30 °C
标题:A Novel Approach For The Synthesis Of Crizotinib Through The Key Chiral Alcohol Intermediate By Asymmetric Hydrogenation Using Highly Active Ir-Spiro-Pap Catalyst
作者:Qian,Jian-Qiang; Et Al
参考文献:Tetrahedron Letters 日期:2014 卷标:55(9) 页码:1528-1531]
877399-50-3 + 185990-03-8 = 877399-74-1
反应条件:1.1 Reagents: Potassium Methoxide Solvents: Methyl Ether; 1 H,30 °C
标题:Boryl Substitution Of Functionalized Aryl-,Heteroaryl- And Alkenyl Halides With Silylborane And An Alkoxy Base: Expanded Scope And Mechanistic Studies
作者:Yamamoto,Eiji; Et Al
参考文献:Chemical Science 日期:2015 卷标:6(5) 页码:2943-2951]
877399-50-3 + 73183-34-3 = 877399-74-1
反应条件:1.1 Reagents: Potassium Acetate Catalysts: (Sp-4-3)-Rel-(Methanesulfonato-Ko)[2′-[(R)-Methylamino-Kn][1,1′-Biphenyl]-2-Yl-K... Solvents: Tetrahydrofuran; 24 H,80 °C
标题:A Monophosphine Ligand Derived From Anthracene Photodimer: Synthetic Applications For Palladium-Catalyzed Coupling Reactions
作者:Wang,Xin; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(20) 页码:8158-8163]
1195-66-0 + 877399-73-0 = 877399-74-1
反应条件:1.1 Reagents: Chloro(1-Methylethyl)Magnesium Solvents: Tetrahydrofuran; 255 Min,-10 °C; -10 °C -> 20 °C; 1 H,20 °C1.2 Solvents: Tetrahydrofuran; 105 Min,20 - 30 °C; 9 H,25 °C
标题:Fit-For-Purpose Development Of The Enabling Route To Crizotinib (Pf-02341066)
作者:De Koning,Pieter D.; Et Al
参考文献:Organic Process Research & Development 日期:2011 卷标:15(5) 页码:1018-1026]
1195-66-0 + 877399-73-0 = 877399-74-1
反应条件:1.1 Reagents: Chloro(1-Methylethyl)Magnesium Solvents: Tetrahydrofuran; -10 °C; 2 H,Rt1.2 -
标题:Improved Synthesis Of Crizotinib
作者:Zhang,Guang-Yan; Et Al
参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2014 卷标:24(6) 页码:445-449]
1195-66-0 + 877399-50-3 = 877399-74-1
反应条件:1.1 Reagents: Chloro(1-Methylethyl)Magnesium Solvents: Tetrahydrofuran; 12 H,20 - 30 °C1.2 Solvents: Tetrahydrofuran; 6 H,20 - 30 °C
标题:A Novel Approach For The Synthesis Of Crizotinib Through The Key Chiral Alcohol Intermediate By Asymmetric Hydrogenation Using Highly Active Ir-Spiro-Pap Catalyst
作者:Qian,Jian-Qiang; Et Al
参考文献:Tetrahedron Letters 日期:2014 卷标:55(9) 页码:1528-1531]
269410-08-4 = 877399-74-1
反应条件:1.1 Reagents: Potassium Carbonate Solvents: Acetonitrile; Reflux
标题:Discovery Of Potent And Orally Effective Dual Janus Kinase 2/flt3 Inhibitors For The Treatment Of Acute Myelogenous Leukemia And Myeloproliferative Neoplasms
作者:Yang,Tao; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2019 卷标:62(22) 页码:10305-10320
叔-丁基氯甲酸酯置于4-二甲氨基吡啶,Sodium Hydride,三乙胺体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 4-[4-(4,4,5,5-四甲基-1,3,2-二氧杂环戊硼烷-2-基)-1H-吡唑-1-基]哌啶-1-甲酸叔丁酯
参考文献:一种克里唑替尼中间体制备方法
标题:一种克里唑替尼中间体制备方法
摘要:本发明为抗肿瘤分子靶向药物克里唑替尼的合成方法,属于制药领域.涉及一种克里唑替尼中间体的合成方法,包括两种还原工艺,一种溴代反应工艺,反应步骤如下:还原工艺一:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶与连二硫酸钠,在机械化学条件下发生还原反应,反应生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;还原工艺二:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶溶于有机溶剂中,催化加氢,还原反应生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;溴代反应工艺:将上述化合物与过硫酸氢钾和溴化盐反应,得到克里唑替尼中间体.该工艺成本低,原材料易购买,操作简便安全,收率高,适用于大规模生产.
海关参考信息
- 2905122000-异丙醇
2905143000-叔丁醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇 - 💡 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:CN-118324790-A
优先权日:2024-04-16
标 题 :A method for photocatalytic synthesis of crizotinib intermediates
专利号:US-2013072495-A1
优先权日:2010-05-14
标 题 :Fused bicyclic kinase inhibitors
发明人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G
权利人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.
专利号:US-8785632-B2
优先权日:2004-08-26
标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
发明人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE
权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER
摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
专利号:US-9951062-B2
优先权日:2012-12-14
标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P
权利人:ARRIEN PHARMACEUTICALS LLC
摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.
专利号:US-8592448-B2
优先权日:2008-11-20
标题:Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
发明人:CHEN XIN; JIN MELZHONG; KLEINBERG ANDREW; LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; WANG JING
权利人:CHEN XIN; JIN MELZHONG; KLEINBERG ANDREW; LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; WANG JING; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
专利号:US-9604966-B2
优先权日:2013-02-16
标 题 :Crizotinib preparation method
发明人:LI YUANQIANG; QIAN JIANQIANG; CHE DAQING
权利人:ZHEJIANG JIUZHOU PHARM CO LTD; ZHEJIANG JIUZHOU PHARM CO LTD
摘要:The present invention relates to the technical field of medicine and organic synthesis, particularly to a method for preparing crizotinib. The method comprises the compound of formula b and the compound of formula e undergoing Suzuki coupling reaction to produce the compound of formula a which then was subjected to deprotection to afford (±) crizotinib.