专利号:US-6852855-B2 优先权日:1999-04-19 标 题 :Synthesis of piperazine ring 发明人:DOLITZKY BEN-ZION 权利人:TEVA PHARMA 摘要:A novel process for preparing a compound of the formula I: n n nwhereinn nR 1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R 2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R 3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.
专利号:WO-2016118586-A1 优先权日:2015-01-20 标 题 :Lowcost, high yield synthesis of nevirapine 发明人:AHMAD SAEED; GUPTON FRANK; VERGHESES JENSON; MCQUADE TYLER 权利人:UNIV VIRGINIA COMMONWEALTH 摘要:Improved methods of producing the HIV drug substance, nevirapine are provided. The methods employ a cost effective and high yield synthetic methods for preparing the nevirapine building block 2-chloro-3-amino-4-picoline (CAPIC) and 2-cyclopropyl amino nicotinate (Me-CAN), and improvements in other steps of nevirapine synthesis.
专利号:US-6603003-B2 优先权日:2000-11-07 标 题 :Method for the preparation of piperazine and its derivatives 发明人:SEBASTIAN SONNY; PATEL HETAL VIRENDRA; THENNATI RAJAMANNAR 权利人:SUN PHARMACEUTICAL IND LTD 摘要:A novel method for the synthesis of piperazine and its derivatives of formula 1,wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms;R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; andR2 is selected from hydrogen, or a methyl group, or a fluoromethyl group;comprising the steps:a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; andb. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.
专利号:US-11718596-B2 优先权日:2014-03-19 标题 :Amyloid targeting agents and methods of using the same 发明人:YANG JERRY; THEODORAKIS EMMANUEL A; SARRAF STELLA 权利人:UNIV CALIFORNIA; AMYDIS INC 摘要:Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
专利号:US-5204478-A 优先权日:1992-08-20 标题 :Process for the synthesis of 2,6-dichloro-5-fluoronicotinic acid and 2,6-dichloro-5-fluoronicotinoyl chloride 发明人:JENNINGS REX A 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 2,6-dichloro-5-fluoronicotinoyl chloride is described where a 2,6-dihydroxy-5-fluoronicotinic acid ester is converted in one step using phosphorus oxychloride and a lithium reagent to 2,6-dichloro-5-fluoronicotinoyl chloride and subsequent basic hydrolysis affords 2,6-dichloro-5-fluoronicotinic acid.
专利号:US-2002035256-A1 优先权日:1999-04-19 标题:Novel synthesis of piperazine ring
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 243. 摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 660.