专利号:WO-2021038581-A1 优先权日:2019-08-30 标题 :A one step synthesis of 2-substituted benzo[b]thiophenes 发明人:SEKAR GOVINDASAMY; POONGUZHALI ELAMVAZHUTHI 权利人:INDIAN INST TECH MADRAS 摘要:The invention pertains to a one step synthesis of 2-substituted benzo[ b ]thiophene of general formula wherein the synthesis of 2-substituted benzo[ b ]thiophenes is by reacting the starting materials substituted or unsubstituted 2-halogenobenzaldehyde and substituted or unsubstituted acetyl/phenacyl bromide with a catalyst, a sulphur source and phase transfer catalyst in an aqueous medium with atmospheric air and at temperature in the range of 25°C-30°C.
专利号:US-11459549-B2 优先权日:2018-05-10 标 题:Method for biocatalytic synthesis of Sitagliptin and intermediate thereof 发明人:WU FAHAO; YANG WEN; LI GANG; SHI HONGWEI; GAO YANGZHE; LIU LILI; YUAN ZHIFA 权利人:CHINA FORTUNE WAY COMPANY; NANJING REDWOOD FINE CHEMICAL CO LTD 摘要:Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.
专利号:US-4739073-A 优先权日:1983-11-04 标题:Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof 发明人:KATHAWALA FAIZULLA G 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein one of R and Ro is and the other is primary or secondary C1-6alkyl not containing an asymmetric carbon atom, C3-6cycloalkyl or phenyl(CH2)m-, wherein R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy, and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C3-6cycloalkyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH-, wherein n is 0, 1, 2 or 3, and Z is wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, benzyl or M, wherein M is a pharmaceutically acceptable cation, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level, and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-3742080-A 优先权日:1969-04-11 标 题 :Rhodium based catalysts for the synthesis of 1,4-dienes 发明人:SU A 权利人:DU PONT 摘要:Improved catalysts are provided for the synthesis of 1,4-dienes from Alpha -monoolefins and conjugated dienes. The catalysts are rhodium (III) salts in combination with amides, phosphoramides, phosphine oxides, or water. The improved catalysts allow control of the trans-cis ratio of the 1,4-diene formed and are operable at useful rates in a wide range of solvent systems, both protonic and aprotic.
专利号:US-9695188-B2 优先权日:2013-12-06 标 题 :Methods useful in the synthesis of halichondrin B analogs 发明人:HU YONGBO; ZHANG HUIMING; CHIBA HIROYUKI; KOMATSU YUKI; LEWIS BRYAN M 权利人:EISAI R&D MAN CO LTD 摘要:In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
专利号:WO-2015130660-A1 优先权日:2014-02-25 标题 :Synthesis of racemic amphetamine derivatives by cuprate addition reaction with aziridine phosphoramidate compounds 发明人:MECKLER HAROLD; GREGG BRIAN THOMAS; YANG JIE 权利人:Chemapotheca LLC 摘要:The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.
摘要:Shimizu, T., Science of Synthesis Knowledge Updates, (2011) 1, 493. 摘要:Marsden, S. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 597. 摘要:Arzneimittel-Forschung. Drug Research., 28(1571), 1978 [] 摘要:Hawley, G.G. The Condensed Chemical Dictionary. 9th ed. New York: Van Nostrand Reinhold Co., 1977., p. 285 摘要:Weast, R.C. (ed.). Handbook of Chemistry and Physics. 60th ed. Boca Raton, Florida: CRC Press Inc., 1979., p. C-84