欧盟法规
C&L通报上下游产品
1,1'-dilithioferr°Cene phenylthiodiphenylphosphine phenyllithium chloro-diphenylphosphine 3-ethoxypropanal ethoxypropionaldehyde (1,1'-bis(diphenylphosphino)ferr°Cene)palladium(II) dichloride palladium合成工艺路线路线简述
- 合成目标产物 1,1'-Bis(Diphenylphosphino)Ferrocene 主要起始原料 Ferrocene, 1,1'-Bis(Diphenoxyphosphino)-
- (文献来源)合成步骤主要原料 Ferrocene, 1,1'-Bis(Diphenoxyphosphino)-
1,1'-双(二苯基膦基)-二茂铁置于bis(2-Chlorophenyl)Borinic Acid,苯硅烷体系中,用 甲苯 用作溶剂,化学反应 18.0H,以71%的收率获得1,1'-双(二苯基膦)二茂铁
参考文献:使用硼酸预催化剂与氢化硅烷的无金属还原膦氧化物,亚砜和n-氧化物
标题:使用硼酸预催化剂与氢化硅烷的无金属还原膦氧化物,亚砜和n-氧化物
摘要:还原至澄清:通过使用双(2-氯苯基)硼酸/苯基硅烷可实现氧化膦,亚砜和n-胺氧化胺的还原.该反应可耐受各种各样的底物,并且可以在温和的条件下以仅2.5Mol%的催化剂负载量进行.NMR光谱表明,硼氢化物是关键的还原物种,因此,必须将双(2-氯苯基)硼酸视为前催化剂.
Doi:10.1002/cctc.201700986
专利信息
专利号:US-11465970-B2
优先权日:2017-12-14
标题 :Method for synthesis of Roxadustat and intermediate compounds thereof
发明人:XU YONGXIANG
权利人:NANJING CAVENDISH BIO ENGINEERING TECH CO LTD; XU YONGXIANG; NANJING CAVENDISH BIO ENG TECH CO LTD
摘要:The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Herein, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description
专利号:WO-2024183094-A1
优先权日:2023-03-07
标 题 :Use of ligand catalyst in synthesis of indole alkaloids
发明人:YAN PUCHA; Cheng Houan; ZHOU BO; HUA YUNYU; SUN ZEBIN; FU XINGFENG; LI YUANQIANG
权利人:ZHEJIANG JIUZHOU PHARM CO LTD
摘要:The present invention provides use of a ligand catalyst in the synthesis of indole alkaloids. The ligand catalyst is formula (1). A method for the catalytic synthesis of the indole alkaloids comprises the following steps: sequentially adding reactants, a metal catalyst, a ligand catalyst, an oxidizing agent, and an additive into a reaction container, adding an organic solvent, carrying out the reaction, and carrying out separation and purification to obtain an indole derivative. The chemical reaction formula of the indole derivative is as follows: formula (2), wherein R1 is selected from one of hydrogen, alkyl, alkoxy, and aryl, R2 is selected from one of trifluoromethanesulfonyl, p-toluenesulfonyl, hydrogen, and alkyl, R3 is selected from one of alkyl, alkoxy, aryl, and heteroaryl, and R4 is selected from one of hydrogen, alkyl, alkoxy, aryl, and heteroaryl. The present invention solves the problem of low yield due to C(sp3)–H bonds being difficult to activate, and generates C-H bonds activated by means of the ligand, thereby reducing by-products.
专利号:US-9783519-B2
优先权日:2015-06-18
标 题:Palladium/silver co-catalyzed tandem reactions synthesis of phenylacetophenone derivatives by oxabenzonorbornadienes with terminal alkynes and their anti-tumor or anti-cancer activities
发明人:BIAN ZHAOXIANG; LIN CHENGYUAN; MU HUAIXUE; FAN BAOMIN; ZHOU YONGYUN; CHEN JINGCHAO; LU AIPING; CHAN ALBERT SUN-CHI
权利人:UNIV HONG KONG BAPTIST UNIV; UNIV YUNNAN MINZU
摘要:This invention relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds. More particularly, it relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds comprising phenylacetophenone derivatives using oxabenzonorbornadienes with terminal alkynes.
专利号:US-7148356-B2
优先权日:2001-07-13
标题:Process for the catalytic synthesis of biaryls and polymers from aryl compounds
发明人:SMITH III MILTON R; MALECZKA ROBERT E
权利人:UNIV MICHIGAN STATE
摘要:A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO 2 CF 3 ), or nonaflate (OSO 2 C 4 F 9 ). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.
专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-12240835-B2
优先权日:2018-09-18
标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity
发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI
权利人:TERNS PHARMACEUTICALS INC
摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.