CAS: 85068-27-5; 2,5-Difluorophenylacetic Acid

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CAS号367-23-7 1,2,4-三氟苯 | CAS号29270-33-5 α-溴-4-氟苯乙酸 | CAS号220259-72-3 α-bromo-(2,5-di... | CAS号767352-24-9 4-(2,5-difluoro... | CAS号662138-60-5 ETHYL(2,5-DIFLU...

1,2,4-三氟苯置于n-甲基吡咯烷酮,Sodium Hydroxide,Sodium Hydride体系中,化学反应 48.0H,反应生成 2,5-二氟苯乙酸
参考文献:Synthesis Of Dihalophenylacetic Acids Using Aromatic Nucleophilic Substitution Strategy
标题:Synthesis Of Dihalophenylacetic Acids Using Aromatic Nucleophilic Substitution Strategy
摘要:一种简单的合成策略被开发用于二卤苯乙酸,特别是3,5-二氟苯乙酸,这是一种重要的药物中间体.通过使用乙基氰乙酸酯的阴离子对二卤氟苯进行芳香亲核取代反应,得到了乙基二卤苯氰乙酸酯.对乙基二卤苯氰乙酸酯进行基础脱羧反应,产生了目标二卤苯乙酸.
DOI:10.1055/s-1997-1385

专利信息

专利号:US-2009123983-A1
优先权日:2007-10-03
标 题:Processes for preparing an intermediate of sitagliptin via enzymatic reduction
发明人：NIDDAM-HILDESHEIM VALERIE
权利人:NIDDAM-HILDESHEIM VALERIE
摘要:The invention provides enzymatic reduction processes for the preparation of 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, particularly, (S)-methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, a key intermediate in the synthesis of Sitagliptin, and the (S)- and (R)-enantiomers of methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate in high enantiomeric purity.

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:EP-0946499-B1
优先权日:1996-11-22
标 题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK NORMAN; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R<1> is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R<2> is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R<3> and R<3'> are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R<7>)n(W)p, wherein R<7> is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH( phi )CH2C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R<1> to -CX'X''-, oxygen and sulfur.

专利号:US-6849650-B2
优先权日:1998-02-27
标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES
权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:EP-0951464-B1
优先权日:1996-11-22
标题:N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; THORSETT EUGENE D; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; JOHN VARGHESE; FANG LAWRENCE Y; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:EP-0951466-B1
优先权日:1996-12-23
标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.