专利号:US-6172205-B1 优先权日:1997-12-11 标题 :Synthetic process toward total synthesis of eleutherobin and its analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; CHEN XIAO-TAO; GUTTERIDGE CLARE E; BHATTACHARYA SAMIT K; ZHOU BISHAN 权利人:TRUSTEES OF COLUMBIA IN THE CI 摘要:This invention provides a process for the preparation of a Eleutherobin derivative of the formula: n wherein R 1 is a hydrogen, ester, nitrile or C 2 H 4 —R wherein R 4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R 2 is a linear or branched alkyl moiety, R 3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R 4 is a hydrogen or CH 2 ,position C 2 and C 3 is cis or trans,position C 8 is α or β and a compound is produced having the structures: n Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-8193180-B2 优先权日:2007-01-24 标 题 :N-amino tetrahydrothiazine derivatives, method of manufacture and use 发明人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE 权利人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE; WOMEN & INFANTS HOSPITAL 摘要:This invention comprises the innovative synthesis of N-amino tetrahydrothiazine free bases and their salts. This invention further comprises the use of the derivatives and their therapeutic application as anticancer agents. Further this invention comprises their manufacture and use.
专利号:WO-2007141253-A1 优先权日:2006-06-07 标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines 发明人:PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-5149838-A 优先权日:1991-09-20 标 题:Intermediates for substituted azetidinones useful as anti-inflammatory and antidegenerative agents 发明人:HUMPHREY GUY R; MADAR ANN M; THOMPSON ANDREW S 权利人:MERCK & CO INC 摘要:Disclosed is a process for the enantioselective synthesis of the compound of Formula I and related compounds. The process comprises the synthesis of the benzofuranyl carboxaldehyde; introduction of the benzylic amine functionality with control of the absolute stereochemistry; preparation of the azetidinone fragment and its coupling to the benzofuranyl amine fragments. The carboxylic acid in Formula I is liberated using heterogenous palladium catalyzed de-allylation of the allyl esters. Compounds I have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents. ##STR1##
专利号:US-8043786-B2 优先权日:2003-03-05 标题 :Acid generators, sulfonic acids, sulfonyl halides, and radiation sensitive resin compositions 发明人:EBATA SATOSHI; WANG YONG; NISHIMURA ISAO 权利人:JSR CORP 摘要:The invention provides novel acid generators which are unproblematic in combustibility and accumulation inside the human body and can generate acids having high acidities and high boiling points and exhibiting properly short diffusion lengths in resist coating films and which permit the formation of resist patterns excellent smoothness with little dependence on the denseness of a mask pattern; sulfonic acids generated from the acid generators; sulfonyl halides useful as raw material in the synthesis of the acid generators; and radiation-sensitive resin compositions containing the acid generators. The acid generators have structures represented by the general formula (I), n nwherein R 1 is a monovalent substituent such as alkoxycarbonyl, alkylsulfonyl, or alkoxysulfonyl; R 2 to R 4 are each hydrogen or alkyl; k is an integer of 0 or above; and n is an integer of 0 to 5. Among the radiation-sensitive resin compositions, a positive one contains a resin having acid-dissociable groups in addition to the above acid generator, while a negative one contains an alkali-soluble resin and a crosslinking agent in addition to the acid generator.
摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 357. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 192. 摘要:Undheim, K., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 743. 摘要:Shen, Q.; Guo, F.; Hartwig, J. F., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 184. 摘要:Kwiecień, H. U., Science of Synthesis: Knowledge Updates, (2024) 3, 183.