2-氟苯酚置于sodium Hydroxide,乙酸酐体系中,用100%的收率获得产物2-氟苯乙酸 参考文献:Spiro(2H-1-Benzopyran-2,4-Piperidine)Derivatives As Glycine Transport Inhibitors 标题:Spiro(2H-1-Benzopyran-2,4-Piperidine)Derivatives As Glycine Transport Inhibitors 摘要:本发明涉及一种具有通式(i)的螺环[2H-1-苯并吡咯烷]衍生物,其中取代基r1,R2,X和y如索权中所定义,或其药学上可接受的盐.该发明还涉及包含所述衍生物的药物组合物,以及在治疗中使用这些螺环[2H-1-苯并吡咯烷]衍生物,更具体地用于治疗中枢神经系统疾病.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
专利号:US-10913747-B2 优先权日:2017-07-04 标题 :Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid 发明人:DE LUCCHI OTTORINO; PADOVAN PIERLUIGI; BRASOLA ELENA 权利人:FIS FABBRICA ITALIANA SINTETICI SPA; F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
专利号:US-11174266-B2 优先权日:2018-02-13 标 题 :Efficient process for the preparation of sitagliptin 发明人:SHI TERRY; LOU SAM; DE LUCCHI OTTORINO; PADOVAN PIERLUIGI 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
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.
[参考文献]: Jonathan M Fitzsimmons, Et Al. Synthesis And σ1 Receptor Binding Of Halogenated N,N'-Diphenethylethylenediamines. Med Chem (Los Angeles). 2011 Dec 25;1(102):1000102.
合成参考文献
摘要:Zhang, M.; Su, W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 96. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 402. 摘要:Schiltz, P.; Gosmini, C., Science of Synthesis: Special Topics, (2021) 1, 91.