专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:US-8637695-B2 优先权日:2011-12-30 标 题:Synthesis of organohalosilane monomers from conventionally uncleavable Direct Process Residue 发明人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID 权利人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID; MOMENTIVE PERFORMANCE MAT INC 摘要:Disclosed herein is a catalytic process for the synthesis of organohalosilane monomers from tetraorganodihalodisilanes and other compounds that are not cleaved during the conventional hydrochlorination of Direct Process Residue. The process is characterized by the use of a catalyst containing (1) one or more heterocyclic amines and/or one or more heterocyclic ammonium halides, and (2) one or more quaternary Group 15 onium compounds.
专利号:US-6472534-B2 优先权日:1999-10-21 标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K 权利人:AGOURON PHARMA 摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
专利号:US-7855285-B2 优先权日:2005-06-14 标 题:Methods for selective N-9 glycosylation of purines 发明人:ROBINS MORRIS J; ZHONG MINGHONG 权利人:UNIV BRIGHAM YOUNG 摘要:A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.
专利号:US-6204398-B1 优先权日:1996-08-23 标题 :Preparation of cyclohexene carboxylate derivatives 发明人:KENT KENNETH M; KIM CHOUNG U; MCGEE LAWRENCE R; MUNGER JOHN D; PRISBE ERNEST J; POSTICH MICHAEL J; ROHLOFF JOHN C; KELLY DAPHNE E; WILLIAMS MATTHEW A; ZHANG LIJUN 权利人:GILEAD SCIENCES INC 摘要:The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
专利号:US-8697901-B2 优先权日:2011-12-30 标题 :Synthesis of organohalosilane monomers via enhanced cleavage of direct process residue 发明人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID 权利人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID; MOMENTIVE PERFORMANCE MAT INC 摘要:Discloses herein is a catalytic process for producing organohalosilane monomers from a high-boiling residue resulting from the Direct Reaction of an organohalide with silicon. The high-boiling residue contains more conventionally cleavable compounds than conventionally uncleavable compounds. The process includes heating the residue in the presence of a catalyst comprising (1) one or more heterocyclic amines and/or one or more heterocyclic ammonium halides, and (2) one or more quaternary Group 15 onium compounds.
[参考文献]: Sylwia Godlewska, Et Al. Bromidotetra-Kis-(2-Isopropyl-1H-Imidazole-κn)Copper(Ii) Bromide. Acta Crystallogr Sect E Struct Rep Online. 2011 Oct 1;67(Pt 10):M1338.
合成参考文献
摘要:Aitken, R. A.; Meehan, A., Science of Synthesis Knowledge Updates, (2014) 3, 187. 摘要:Banert, K., Science of Synthesis Knowledge Updates, (2015) 2, 260.