专利号:WO-2009064476-A1 优先权日:2007-11-13 标 题 :Preparation of sitagliptin intermediate 发明人:PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 权利人:TEVA PHARMA; TEVA PHARMA; PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 摘要:Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.
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:US-2009192326-A1 优先权日:2007-11-13 标题 :Preparation of sitagliptin intermediate 发明人:PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 权利人:PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 摘要:Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.
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-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-6416861-B1 优先权日:1999-02-16 标题 :Organosilicon compounds and uses thereof 发明人:LEE YOUNGHEE; SILVERMAN RICHARD B 权利人:UNIV NORTHWESTERN 摘要:A compound of the formula: n and a resin-bound compound of the formula: n and their use in combinatorial chemistry and in the synthesis of compounds comprising at least one aromatic moiety is described, where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , L 1 , P, Ar 1 , and X are as herein defined.