专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-8273790-B2 优先权日:2005-01-14 标 题:Exo-selective synthesis of himbacine analogs 发明人:THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D 权利人:THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D; SCHERING CORP 摘要:This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-5512701-A 优先权日:1995-06-07 标题:Process for the synthesis of vinyl sulfenic acid derivatives 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo[b]thiophenes, in particular 2-aryl-benzo[b]thiophenes.
专利号:US-2012203004-A1 优先权日:2009-08-13 标题 :process for the synthesis of alkyl/aralkyl (2s)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof: key intermediates for the preparation of dppiv inhibitors 发明人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA 权利人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA; LUPIN LTD 摘要:An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.
专利号:US-8697876-B2 优先权日:2010-04-02 标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 发明人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN 权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC 摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).
参考文献:10.1007/s00894-011-1169-2 摘要:Singh DV, Adeppa K, Misra K. Mechanism of isoproturon resistance in Phalaris minor: in silico design, synthesis and testing of some novel herbicides for regaining sensitivity. Journal of Molecular Modeling. 2011 Jul 15;18(4):1431–45. doi: 10.1007/s00894-011-1169-2.