专利号:US-2024287126-A1 优先权日:2021-05-14 标 题:Novel synthesis of cholesterol 发明人:SCHINZER DIETER; SPIESS OLIVER; MUNT MAXIM; INDOLESE ADRIANO; ROUX LIONEL 权利人:CORDENPHARMA INT GMBH; UNIV OTTO VON GUERICKE MAGDEBURG; CORDENPHARMA INT 摘要:The invention relates to a synthesis of cholesterol; a ring opening step of the compound of formula (I) and subsequent activation and reduction step yielding cholesterol. The inventions relates also to intermediates achieved during said synthesis.
专利号:US-5554725-A 优先权日:1994-09-14 标题:Synthesis of dolastatin 15 发明人:PETTIT GEORGE R 权利人:UNIV ARIZONA 摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.
专利号:US-4978744-A 优先权日:1989-01-27 标题:Synthesis of dolastatin 10 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.
专利号:US-6248865-B1 优先权日:1994-05-06 标 题:Compounds useful for the synthesis of dolastatin analogs 发明人:AMBERG WILHELM; BERNARD HARALD; BUSCHMANN ERNST; HAUPT ANDREAS; JANITSCHKE LOTHAR; JANSSEN BERND; KARL ULRICH; KLING ANDREAS; MUELLER STEFAN; DE POTZOLLI BERND; RITTER KURT; THYES MARCO; ZIERKE THOMAS 权利人:BASF AG 摘要:Compounds of the formulawhere R1, R2, R3 and R4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.
专利号:AU-2022273995-A1 优先权日:2021-05-14 标题:Novel synthesis of cholesterol
专利号:US-9669015-B2 优先权日:2005-04-07 标题 :Piperidine-2, 6-dione derivatives and their use as tumor necrosis factor inhibitors 发明人:ZHANG HESHENG 权利人:TIANJIN HEMAY BIO-TECH CO LTD 摘要:This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNFα releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): n nwherein n represents 1, 2, 3, 4, 5 or 6; R 1 represents from one to four of the same or different substituents selected from F, Cl, Br, C 1-4 alkyl, OH, OC 1-4 alkyl, NO 2 , NHC(O)C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 ; R 2 represents OR 3 , NR 3 R 4 , N(R 3 )COR 4 , O 2 CR 5 ; R 3 and R 4 represent independently and at each occurrence H or C 1-4 alkyl; R 5 represents CHR 6 NR 7 R 8 , CHR 6 NR 9 C(O)CHR 10 NR 7 R 8 , a heterocycle W or CHR 6 NR 9 C(O)W; R 6 , R 9 , R 10 represent independently and at each occurrence H, or C 1-4 alkyl; R 7 and R 8 represent independently and at each occurrence H, C 1-4 alkyl, or R 7 and R 8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-membered, five-membered, six-membered, seven-membered, or eight-membered saturated or unsaturated heterocycle.
参考标题:Synthesis Of Yb Complexes With Amino-Acid-Armed Ligands For Direct Asymmetric Tandem Aldol Reduction Reactions 作者:Maciej Stodulski,Jarosław Jaźwiński,Jacek Mlynarski |发布日期:2008.11 摘要:Amino Acids. In This Article, The Asymmetric Aldol-Reduction Reaction Leading To 1,3-Diols (Known As The Aldol-Tishchenko Reaction) Has Been Performed With An Elaborated Family Of Ligands. This Unique Tandem Reaction Was Catalysed By Chiral Yb Complexes That Promote Both The Aldol Reaction Of Unactivated Carbonyl Compounds And The Evans-Tishchenko Reduction Of The Aldol Intermediates. 1,3-Anti-Diols With
合成参考文献
参考文献:10.1021/ol048900y 摘要:Tsuda M, Kasai Y, Komatsu K, Sone T, Tanaka M, Mikami Y, Kobayashi J. Citrinadin A, a Novel Pentacyclic Alkaloid from Marine-Derived Fungus Penicillium citrinum. Org. Lett. 2004 Aug 11;6(18):3087–9. doi: 10.1021/ol048900y.