磷酸三(三甲基硅基)酯置于sodium Azide体系中,化学反应 0.17H,以87%的收率获得产物叠氮基三甲基硅烷 参考文献:Lazukina,L. A.; Kukhar,V. P.,Journal Of General Chemistry Of The Ussr,1990,Vol. 60,# 3.2,P. 608 标题:Lazukina,L. A.; Kukhar,V. P.,Journal Of General Chemistry Of The Ussr,1990,Vol. 60,# 3.2,P. 608
专利信息
专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
专利号:WO-8800592-A1 优先权日:1986-07-18 标题:DIASTEROSELECTIVE STRECKER SYNTHESIS OF alpha-AMINOACIDS FROM GLYCOSYLAMINE DERIVATES 发明人:KUNZ HORST; SAGER WILFRIED; PFRENGE WALDEMAR; DECKER MATHIAS 权利人:CELAMERCK GMBH & CO KG 摘要:O-acyl-protected glycosylamines, in particular 2,3,4,6-tetra-O-pivaloyl-beta-D-galactopyranosylamine (1), their preparation and their use for the diastereoselective synthesis of alpha-aminoacids. With compounds such as (1), one can obtain by Strecker synthesis high yields and high diastereomer surplus. The direction of the asymmetric induction can be determined by the selection of the solvent. This type of synthesis is particularly effective when carried with Lewis acid catalysts. One obtains also high yields and high diastereoselectivity during Ugi four component synthesis facilitated by Lewis acids by using amines such as (1).
专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-4910310-A 优先权日:1988-10-03 标 题:Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 发明人:CAMPBELL ARTHUR L; BEHLING JAMES R; BABIAK KEVIN A; NG JOHN S; MUELLER RICHARD A; FLEET GEORGE W J 权利人:SEARLE & CO 摘要:Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-ω-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.
专利号:US-9233943-B2 优先权日:2012-01-10 标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir 发明人:GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.
专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.