专利号:EP-1724260-B1 优先权日:2005-05-06 标题:Process for the synthesis of (2S, 3aR, 7aS)octahydroindole-2-carboxylic acid and its conversion to trandolapril 发明人:AKHTAR HAIDER; RAMESH BABU POTLURI; VENKATA SUBHRAMANIAN HARIHARAK; HARI PRASSAD KODALI 权利人:SOCHINAZ SA 摘要:The present invention describes a novel method for the synthesis of (2S,3aR,7aS)-octahydroindole-2-carboxylic acid of formula III nusing a new intermediate of formula II nand conversion of the product of formula-III to trandolapril of formula I
专利号:US-2023303611-A1 优先权日:2022-01-21 标题:Synthesis of an antiviral azasugar triphosphate 发明人:KOTIAN PRAVIN L; Dang zhao; WU MINWAN 权利人:BIOCRYST PHARM INC 摘要:Provided are methods of making the active 5′-triphosphate form of galidesivir (compound 1) and the active 5′-triphosphate form of azasugar nucleoside analogues (compound 2):a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively:
专利号:US-2024208900-A1 优先权日:2021-04-16 标题 :Synthesis of dimethyl-c17-32-alkyl sulfonium salts 发明人:STROOT JOERG; ZHERSH SERHII; RIPENKO VASYL 权利人:HELM AG 摘要:The invention relates to a process for the preparation of a dimethyl-C 17-32 -alkyl sulfonium salt, preferably a dimethyl-C 17-32 -alkyl sulfonium halide, more preferably a dimethyl-C 17-32 -alkyl sulfonium chloride, still more preferably dimethyl octadecyl sulfonium chloride, the process comprising the steps of: providing a mixture of a C 17-32 -alkyl halide and dimethyl sulfide; and reacting the C 17-32 -alkyl halide with the dimethyl sulfide.
专利号:US-8680294-B2 优先权日:2009-07-29 标题 :Enantio- and stereo specific synthesis of β-amino-α-hydroxy amides 发明人:TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO 权利人:TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO; MERCK SHARP & DOHME 摘要:Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
专利号:US-6011171-A 优先权日:1996-08-14 标 题 :Process for synthesis of tertiary carboxylic acids and the esters thereof 发明人:XU QIANG; SOUMA YOSHIE 权利人:JIRO HIRAISHI DIRECTOR GENERAL 摘要:The present invention provides a process for synthesizing tertiary carboxylic acids or the esters thereof having one or two more carbon atoms than the raw material has, comprising reacting in a strong acid (e.g., sulfuric acid, sulfuric acid-phosphoric acid, hydrogen fluoride, fluorosulfuric acid, boron trifluoride.water complex and trifluoromethanesulfonic acid) a raw material compound (i.e., olefin, alcohol, diene, diol or saturated hydrocarbon) with carbon monoxide in the presence of a specific metal carbonyl catalyst (i.e., platinum carbonyl catalyst, palladium carbonyl catalyst and gold dicarbonyl catalyst). The metal carbonyl catalyst is formed by reacting in a strong acid at least one specific metal compounds (e.g., platinum compound such as platinum (II, IV) oxide, platinum (II, IV) hydroxide, a platinum powder, etc.; palladium compound such as palladium (II, III, IV) oxide, palladium (II) hydroxide, palladium (II) sulfate, palladium (II) carboxylate, a palladium powder, etc.; and gold compound such as gold (I, III) oxide, gold (I, III) hydroxide, a gold powder, etc.) with carbon monoxide.
专利号:US-4518602-A 优先权日:1982-10-07 标题 :Vinyl carboxylic acid derivatives, their production and use as inhibitors of thromboxane synthetase 发明人:TERAO SHINJI; NISHIKAWA KOHEI 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:Novel compound of the formula: wherein R1 is a pyridyl group; R2 is a phenyl, thienyl, furyl, naphthyl, benzothienyl or pyridyl group which may have as a substituent a lower alkoxy, a lower alkyl, a halogen, trifluoromethyl, a lower alkenyl or methylenedioxy; R3 is hydrogen, benzyl or a lower alkyl; one of R4 and R5 is hydrogen or a lower alkyl, and the other is an aryloxy, or lower aliphatic hydrocarbon, an alicyclic hydrocarbon having not more than 6 carbon atoms or an aromatic group which may have a substituent, or a group represented by the formula, -S(O)m-R6 (in which R6 is phenyl or a lower alkyl group; m is an integer of 0 to 2), or R4 and R5 each combine with the other to represent one alkylene group; n is an integer of 2 to 6, or a pharmaceutically acceptable salt thereof has a selective inhibitory action on bio-synthesis of thromboxane A2(TXA2) and an effect of enhancing the production of prostaglandin I2(PGI2), and can be used in mammals for to prevention and treatment of arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardian infarction, apoplexy, infarct of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).
摘要:Schobert, R.; Hölzel, C.; Barnickel, B., Science of Synthesis, (2010) 47, 64. 摘要:Wicha, J., Science of Synthesis, (2009) 48, 186. 摘要:Santana, V. C. S.; Munaretto, L. S.; de Lucca, E. C., Jr., Science of Synthesis Knowledge Updates, (2022) 1, 206. 摘要:Witt, D., Science of Synthesis Knowledge Updates, (2011) 3, 306. 摘要:Marsden, S. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 586.