专利号:US-8765668-B2 优先权日:2010-06-04 标 题 :Methods of synthesis of β-aminobutyryl substituted compounds 发明人:STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO 权利人:STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO; LEK PHARMACEUTICALS 摘要:The present invention relates to process to prepare β-aminobutyryl compounds having β-amino acid core structural moieties and optionally having γ-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.
专利号:EP-2397141-A1 优先权日:2010-06-16 标 题:Process for the synthesis of beta-amino acids and derivatives thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to a process for the preparation of β-amino acids and derivatives thereof, which is especially suited for gliptins and particularly sitagliptin. A key step makes use of suitably derivatized epoxides or aziridines, which owing to a chirality provides a source of chirality for intermediates which are suitable for building up β-amino acids and similar compounds, in particular in the construction of the sitagliptin molecule.
专利号:US-2004068141-A1 优先权日:2002-10-08 标 题 :Process for the synthesis of trifluorophenylacetic acids 发明人:ARMSTRONG JOSEPH D; DREHER SPENCER D; IKEMOTO NORIHIRO 摘要:The present invention addresses a process for the preparation of 2,4,5-trifluorophenylacetic acid using a Cu(I) salt as a catalyst.
专利号:US-6870067-B2 优先权日:2002-10-08 标 题 :Process for the synthesis of trifluorophenylacetic acids 发明人:IKEMOTO NORIHIRO; DREHER SPENCER D 权利人:MERCK & CO INC 摘要:The present invention is concerned with a process for the preparation of trifluorophenylacetic acids using a Grignard reagent and an allylating agent, such as allyl bromide.
专利号:US-8471057-B2 优先权日:2009-09-27 标 题:Sitagliptin intermediates, preparation methods and uses thereof 发明人:ZHU GUOLIANG; ZHANG JIAN; YANG LIJUN; YAO QINGDAN; YING JIE 权利人:ZHU GUOLIANG; ZHANG JIAN; YANG LIJUN; YAO QINGDAN; YING JIE; ZHEJIANG JIUZHOU PHARM CO LTD 摘要:The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin. The structures of the compounds mentioned above are as the following:
专利号:US-7205300-B2 优先权日:1997-12-31 标 题:Aryl fused azapolycyclic compounds 发明人:COE JOTHAM WADSWORTH; BROOKS PAIGE ROANNE PALMER 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.