3-甲基噻吩置于溴乙烷,乙醚,Sodium体系中,化学反应生成4-甲基-2-噻吩甲酸 参考文献:Alkylation During Transmetalation Of 3-Methylthiophene 标题:Alkylation During Transmetalation Of 3-Methylthiophene 摘要: Doi:10.1021/ja01127A504
专利号:US-2005085492-A1 优先权日:2003-10-20 标 题:Stereoselective process for the synthesis of chiral garft compounds and intermediates 发明人:RAHMAN LEERA 权利人:AGOURON PHARMACEUTICALS MINC 摘要:The present invention describes a stereoselective preparation of derivatives and precursors of molecules having formula 1: n nMethod of preparing the compounds, intermediates and derivatives are described. The methods described herein allow the preparation of diastereomeric forms of compound having formula 1. The compounds of the invention are GARFT inhibitors.
专利号:US-2004266796-A1 优先权日:2003-06-25 标 题:Convergent processes for the synthesis of a GARFT inhibitor containing a methyl substituted thiophene core and intermediates therefor 发明人:DOVALSANTOS ELENA; FLAHIVE ERIK JON; HALDEN BRIAN JOHN; MITCHELL MARK BRYAN; NOTZ WOLFGANG REINHARD LUDWIG; O'NEILL-SLAWECKI STACY ANN; TIAN QINGPING 权利人:AGOURON PHARMA 摘要:The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: n n n wherein each of R 1 and R 2 are independently a hydrogen atom or a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; from an intermediate of the formula n n n wherein R 3 is a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n Pg 1 is an amino protecting group; n R 4 is H; n or Pg 1 can optionally be taken together with R 4 and the nitrogen to which Pg 1 and R 4 are attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O) j wherein j is an integer from 0 to 2, and —NR 8 —, provided that two O atoms, two S(O) j moieties, or an O atom and a S(O) j moiety are not attached directly to each other; n R 5 is selected from the group consisting of —C≡C— and —CHâ•?CH—; and n R 8 is independently H or C 1 -C 6 alkyl; n to form the compound of the formula (I) that is optically pure; and to processesfor preparing intermediates thereof.
专利号:WO-2004113337-A1 优先权日:2003-06-25 标 题:Convergent synthesis of a garft inhibitor containing a methyl substitute thiophene core and a tetrahydropyrido`2,3-d! pyrimidine ring system and intermediates therefor
专利号:US-4093622-A 优先权日:1975-05-19 标题 :Pyridine esters of cyclopropane-carboxylic acid 发明人:HENRICK CLIVE A; STAAL GERARDUS B 权利人:ZOECON CORP 摘要:Heterocyclic organic esters and thioesters characterized by the presence of one or two cyclopropane moieties, synthesis thereof, and compositions thereof for the control of mites and ticks.
专利号:US-2004043959-A1 优先权日:2002-03-04 标 题 :Combination therapies for treating methylthioadenosine phosphorylase deficient cells 发明人:BLOOM LAURA A; BORITZKI THEODORE J; OGDEN RICHARD; SKALITZKY Donald; KUNG PEI-PEI; ZEHNDER LUKE; KUHN LESLIE; MENG JERRY JIALUN 摘要:The present invention is directed to combination therapies for treating cell proliferative disorders associated with methylthioadenosine phosphorylase (MTAP) deficient cells in a mammal. The combination therapies selectively kill MTAP-deficient cells by administering an inhibitor of de novo inosinate synthesis and administering an anti-toxicity agent, wherein the inhibitors of de novo inosinate synthesis are inhibitors of glycinamide ribonucleotide formyltransferase (“GARFTâ€?) and/or aminoinidazolecarboximide ribonucleotide formyltransferase (“AICARFTâ€?), and the anti-toxicity agent is an MTAP substrate (e.g. methylthioadenosine or “MTAâ€?), a precursor of MTA, an analog of an MTA precursor or a prodrug of an MTAP substrate.
专利号:US-2006211603-A1 优先权日:2004-08-18 标 题:Ramoplanin derivatives possessing antibacterial activity 发明人:RAJU BORE G; CIABATTI ROMEO; MAFFIOLI SONIA I; SINGH UPINDER; ROMANO GABRIELLA; MICHELUCCI ELENA; TISENI PAOLO S; CANDIANI GIANPAOLO; KIM BUM; O'DOWD HARDWIN 权利人:VICURON PHARM INC 摘要:Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
摘要:A. R. Butler, J. Chem. Soc. (B) 1970, 867. 摘要:E. Imoto and R. Motoyama, Bull. Naniwa Univ. 2A, 127 (1954); CA 49, 9614. 摘要:Y. Otsuji, T. Kimura, Y. Sugimoto, E. Imoto, Y. Omori and T. Okawara, Nippon Kagaku Zasshi 80, 1021 (1959). 摘要:Sanz, R.; Su, Science of Synthesis: Knowledge Updates, (2024) 1, 105.