专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-8309716-B2 优先权日:2005-07-29 标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis 发明人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J 权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER 摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
专利号:US-8026383-B2 优先权日:2001-07-06 标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN 权利人:BASF SE 摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
专利号:US-2004152897-A1 优先权日:2002-09-13 标 题 :Synthesis of indolizines 发明人:SUN LIJUN; KOYA KEIZO; XIA ZHI-QIANG; PRZEWLOKA TERESA; ZHANG SHIJIE; ONO MITSUNORI 权利人:SYNTA PHARMACEUTICALS CORP 摘要:Disclosed are methods of preparing substituted indolizines represented by the following formula: n n n comprising reacting a substrate represented by the following formula: n n n with either the cyclization reagent of the following formula: n n n or, a reagent prepared by reacting the compound represented the formula below with an alkylating agent: n n n The variables in the above formulas are defined herein.
专利号:US-11827598-B1 优先权日:2022-07-15 标 题:Preparation method of tofacitinib citrate 发明人:HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han 权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:The present disclosure provides a preparation method of tofacitinib citrate, which comprises the following steps: passing an intermediate TOF-2 into hydrogen at a normal pressure in the presence of a catalyst to obtain an intermediate TOF-3; in the presence of a solvent and a base, under a reduced pressure of −490 mmHg to −760 mmHg, and at a temperature of 10° C. to 25° C., reacting TOF-3 with ethyl cyanoacetate to generate an intermediate TOF-4; heating and dissolving TOF-4 and citric acid in a solvent, and performing separation by cooling to obtain tofacitinib citrate. The present disclosure obtains tofacitinib citrate with high yield, high purity and low impurities by changing a gas flow rate and a reaction temperature and pressure of a hydrogenation reaction. Therefore, the preparation method is suitable for industrial production.
专利号:US-7842834-B2 优先权日:2005-07-21 标 题:Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts 发明人:MICHALAK RONALD S; HELOM JEAN L; ZELDIS JOSEPH 权利人:WYETH LLC 摘要:The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar—(R) z —SO 2 —X and sulfonamides of Formula Ar—(R) z —SO 2 —NR 4 R 5 , where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals.