专利号:US-5849951-A 优先权日:1995-03-01 标题 :Synthesis of carboxylic and hydroxamic acid derivatives 发明人:FLOYD CHRISTOPHER DAVID; WHITTAKER MARK 权利人:BRITISH BIOTECH PHARM 摘要:PCT No. PCT/GB96/00467 Sec. 371 Date Aug. 29, 1997 Sec. 102(e) Date Aug. 29, 1997 PCT Filed Mar. 1, 1996 PCT Pub. No. WO96/26918 PCT Pub. Date Sep. 6, 1996A method for the preparation of a compound of formula (I) (I) wherein X is hydrogen; Y is (i) a group -CO2R5 wherein R5 is a carboxyl protecting group or (ii) a group -CONR6OR7 wherein R6 is an amino protecting group and R7 is a hydroxyl protecting group; and S1, S2, S3 and S4 each represent covalently bound moieties which are substantially non-reactive with the reaction components (II), (III), or (IV) defined below, which method comprises causing the co-condensation in a liquid organic medium of a carboxylic acid reaction component of formula (II); an aldehyde of formula (IIIA); ammonia; and an isonitrile reaction component of formula (IV): (II) (IIIA) (IV) wherein Y, S1, S2, S3 and S4 are as defined with respect to formula (I).
专利号:US-6541276-B2 优先权日:1996-10-28 标题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives and combinatorial libraries thereof 发明人:PATEL DINESH V; NGU KHEHYONG 权利人:VERSICOR INC 摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteases).
专利号:US-7166729-B2 优先权日:2001-08-02 标 题:Process for the preparation of 5-substituted isobenzofurans 发明人:DALL ASTA LEONE; COTTICELLI GIOVANNI 权利人:INFOSINT SA 摘要:There is described a process for the preparation of citalopram and of its pharmaceutically acceptable salts, which comprises treating a 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5 isobenzofurancarbaldoxime, O-substituted preferably with a diphenylmethyl or triphenylmethyl group, with formic-acetic anhydride. Furthermore, the total synthesis of citalopram, as free base or in form of its pharmaceutically acceptable salt, starting from 5-formylphthalide is described.
专利号:WO-9626918-A1 优先权日:1995-03-01 标题:Synthesis of carboxylic and hydroxamic acid derivatives
专利号:WO-9818754-A1 优先权日:1996-10-28 标 题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof
专利号:US-5491167-A 优先权日:1993-01-29 标题 :Hexahydronaphthalene ester derivatives, their preparation and their therapeutic uses 发明人:ISHIHARA SADAO; KOGEN HIROSHI; KOGA TEIICHIRO; KITAZAWA EIICHI; SERIZAWA NOBUFUSA 权利人:SANKYO CO 摘要:Compounds of formula (I): ##STR1## and their salts and esters have the ability to inhibit the synthesis of cholesterol, and can thus be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.
[参考文献]: Francisco J Prado-Prado, Et Al. Multi-Target Spectral Moment Qsar Versus Ann For Antiparasitic Drugs Against Different Parasite Species. Bioorg Med Chem. 2010 Mar 15;18(6):2225-2231. [参考文献]: Vishal Patil, Et Al. Antimalarial And Antileishmanial Activities Of Histone Deacetylase Inhibitors With Triazole-Linked Cap Group. Bioorg Med Chem. 2010 Jan 1;18(1):415-25.
合成参考文献
摘要:Blakemore, P. R., Science of Synthesis, (2005) 21, 871.