专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-6207858-B1 优先权日:1999-03-03 标 题 :Regioselective synthesis of DTPA derivatives 发明人:CHINN PAUL; GYORKOS ALBERT; LABARRE MICHAEL J; RUHL STEVE; RYSKAMP THOMAS 权利人:IDEC PHARMA CORP 摘要:The present invention provides a process for high yield regioselective synthesis of DTPA derivatives that eliminates the need for ion exchange chromotographic separation of intermediates. Moreover, as this process yields a single regioisomer of the chelate, it provides for the regiospecific synthesis of desired chelates useful as radiolabeling agents.
专利号:US-10011580-B2 优先权日:2016-04-21 标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof 发明人:WALSE SPENCER S; KUZMICH DANIEL 权利人:US AGRICULTURE 摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):
专利号:WO-0058264-A1 优先权日:1999-03-26 标 题:Method for the synthesis of non-symmetrical dtpa compounds 发明人:ACHILEFU SAMUEL I; SRINIVASAN ANANTHACHARI 权利人:MALLINCKRODT INC; ACHILEFU SAMUEL I; SRINIVASAN ANANTHACHARI 摘要:The synthesis of compounds of formula (XIV) wherein each R4 is an alkyl group having 1 to 15 carbon atoms, and R6 is a linking moiety having 1 to 10 carbon atoms, is disclosed. These compounds are useful intermediates in the synthesis of compounds of formula (X). These compounds are useful in the preparation of nuclear pharmaceuticals such as those used for tumor imaging or tumor therapy.
专利号:WO-0102339-A1 优先权日:1999-07-01 标题 :Versatile method for the synthesis of iso-dtpa 发明人:ACHILEFU SAMUEL I 权利人:MALLINCKRODT INC; ACHILEFU SAMUEL I 摘要:The synthesis of compounds of formula (XII) is disclosed. These compounds are useful intermediates in the synthesis of compounds of formulae (XI) and (X). These compounds are useful in the preparation of nuclear pharmaceuticals such as those used for tumor imaging or tumor therapy.