CAS: 1878-65-5; 3-Chlorophenylacetic Acid

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3-氯苯乙烯置于葡萄糖,氧气体系中,用 Aq. Phosphate Buffer 用作溶剂,化学反应 10.0H,以81%的收率获得3-氯苯乙酸
参考文献:通过一锅级联生物转化将苯乙烯衍生物的区域和立体选择性氧化为芳烷酸.
标题:通过一锅级联生物转化将苯乙烯衍生物的区域和立体选择性氧化为芳烷酸.
摘要:在化学合成和制造中非常需要绿色和选择性氧化方法.在这项工作中,我们开发了一种生物催化方法,可通过单锅环氧化-异构化-氧化顺序将苯乙烯衍生物区域和立体选择性氧化为芳酸和(S)-2-芳基丙酸.这是通过大肠杆菌(styabc-Ecaldh)的工程化完成的,它可以同时表达苯乙烯单加氧酶(smo),氧化苯乙烯异构酶(soi)和乙醛脱氢酶(ecaldh),作为一种活性且易于获得的全细胞催化剂.使用大肠杆菌对苯乙烯和11个取代的苯乙烯进行区域选择性氧化一次操作即可完成电解槽,以高转化率和高收率生产出12种苯乙酸.共表达smo,Soi和adh9V1(突变的酒精脱氢酶)的大肠杆菌(styabc-Adh9V1)工程导致了能够将α-甲基苯乙烯衍生物区域和立体选择性氧化为相应手性酸的生物催化剂.的4(一锅不对称合成小号)-2-芳基丙酸是在非常好的转化率和非常好的实现ee与大肠杆菌细胞.这是一种新型的不对称烯烃氧化反应
Doi:10.1002/adsc.201700416

专利信息

专利号:US-7026339-B2
优先权日:2003-11-07
标题 :Inhibitors of HCV NS5B polymerase
发明人：YANG FAN; ZHANG BO; WICNIENSKI NANCY ANNE; PFEFFERKORN JEFFREY ALLEN; GREENE MEREDITH L; CHEN KE; NUGENT RICHARD A; REDING MATTHEW TODD; KELLY ROBERT CHARLES; MITCHELL MARK A; FUNK LEE A; HEIER III RICHARD FREDERICK; ANDERSON REBECCA MERRY
权利人:YANG FAN; ZHANG BO; WICNIENSKI NANCY ANNE; PFEFFERKORN JEFFREY ALLEN; GREENE MEREDITH L; CHEN KE; NUGENT RICHARD A; REDING MATTHEW TODD; KELLY ROBERT CHARLES; MITCHELL MARK A; FUNK LEE A; HEIER III RICHARD FREDERICK; ANDERSON REBECCA MERRY
摘要:The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.

专利号:US-4334079-A
优先权日:1980-11-03
标 题:Synthesis of substituted benzyl esters
发明人：GREENE JAMES M; BUNNELL CHARLES A
权利人:LILLY CO ELI
摘要:A process for preparing certain substituted benzyl esters of phenylacetic acids by esterification in a solvent in which the salt of the acid is insoluble, and in the presence of a phase transfer catalyst.

专利号:US-4215044-A
优先权日:1979-04-23
标题:Synthesis of α-fluorocarbonyl compounds
发明人：MIDDLETON WILLIAM J
权利人:DU PONT
摘要:Process for preparing an organic compound of the formula R 2 R 2 CFC(O)R 3 , which process comprises contacting and reacting in a reaction mixture which includes an inert solvent, at a temperature of -40° C. to -100° C., ROF and ##STR1## R is polyfluoroperhaloalkyl of 1-6 carbon atoms or FOCF 2 ; R 1 is hydrocarbyl of 1-6 carbon atoms; n each R 2 is selected from H, alkyl of 1-17 carbon atoms, cycloalkyl of 3-6 carbon atoms, aryl, heteroaryl and such alkyl, cycloalkyl, aryl and heteroaryl substituted by halogen or alkoxy of 1-6 carbon atoms; n R 3 is selected from H, alkyl and haloalkyl of 1-16 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl and haloaryl, OSi(R 1 ) 3 , OH, NH 2 , alkoxy of 1-6 carbon atoms, aryloxy, NHR 1 and NR 1 2 wherein R 1 is alkyl of 1-6 carbon atoms, N-arylamino and nitrogen or sulfur heterocyclic of 4-5 carbon atoms; n R 3 and one R 2 taken together is a diradical which with the Câ•?C group is carbocyclic, heterocyclic or haloheterocyclic, and recovering from the reaction mixture the compound of the formula R 2 R 2 CFC()R 3 .

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.