专利号:US-5115099-A 优先权日:1988-06-14 标 题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates 发明人:KUROIWA KATSUMASA; MATSUURA HITOSHI; KATAYAMA KATSUHIRO; NAKATSUYAMA SHUICHI; NAGASAWA TAKESHI; ENDO KOJI 权利人:NITTO BOSEKI CO LTD 摘要:Novel compounds represented by the following formula: ##STR1## wherein A represents a specific amino acid residue are excellent as substrates for determination of enzyme activity such as trypsin, etc. The compounds can be synthesized from novel arginyl-3-tert-alkyloxycarbonyl-4-nitroanilides by a novel process comprising a selective deprotection step whereby the protecting group on the α-amine group of arginine is removed in the presence of a hydrochloric acid, acetic acid and dimethylformamide mixture, but a tert-alkyl protecting group on the --COOH group of the nitroanilide ring is not removed by this step.
专利号:US-9828386-B2 优先权日:2013-11-15 标题:Sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof 发明人:TANG YAJIE; LI JIANLONG; ZHAO WEI; LI HONGMEI 权利人:UNIV HUBEI TECHNOLOGY 摘要:The present invention discloses a sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof. The present invention introduces a rigid aromatic heterocyclic compound, as well as a further sulfonamidated product of 3-amino-5-mercapto-1,2,4-triazole, 2-amino-5-mercapto-1,3,4-thiadiazole, 4-methylbenzenesulfonyl chloride, or 4-methoxybenzenesulfonyl chloride as a substituent group, into position 4 of the C-ring of podophyllotoxin or 4′-demethylepipodophyllotoxin to obtain the podophyllotoxin derivative shown in formula (V), said derivative having significantly increased antitumor activity and reduced toxic side effects. Experiments on in vitro tumor cell inhibition indicate that the antitumor activity of the compound of formula (V) of the present invention is significantly higher than the antitumor activity of podophyllotoxin or 4′-demethylepipodophyllotoxin.
专利号:CN-108250115-A 优先权日:2018-03-02 标 题 :Method for the coupling synthesis of aryl sulfides from tertiary amines
专利号:EP-0513863-A1 优先权日:1988-06-14 标题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates
专利号:EP-0513863-B1 优先权日:1988-06-14 标题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates
专利号:EP-0347734-A2 优先权日:1988-06-14 标 题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates
参考标题:Thioimides: New Reagents For Effective Synthesis Of Thiolesters From Carboxylic Acids 作者:Adam Henke,Jiri Srogl |发布日期:2008.10.3 摘要:Carboxylic Acids Are Used As The Precursors For The Convenient Synthesis Of Thiolesters In The Phosphine Mediated Process. Cyclic And Acyclic Thioimides Show Equal Efficiency, Furnishing The Desired Thiolesters In Good To Excellent Yields. The General, Highly Efficient Transformation Tolerates Various Functional Groups And The Resulting Thiolesters Are Obtained In High Purity After A Simple Separation. The