专利号:WO-9804535-A1 优先权日:1996-07-26 标 题 :A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 权利人:DU PONT MERCK PHARMA 摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of formula (VI-a) is particularly effective in the treatment of HIV.
专利号:US-6348616-B1 优先权日:1996-07-26 标题 :Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of the formula:is particularly effective in the treatment of HIV.
专利号:US-7842813-B2 优先权日:2008-05-09 标 题 :Processes for the preparation of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine 发明人:TANG DATONG; HAN YINGLIN; HUANG YANHE; PHAN LY TAM; OR YAT SUN; WANG ZHE 权利人:ENANTA PHARM INC 摘要:The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):
专利号:US-7820858-B2 优先权日:2006-03-25 标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation 发明人:CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.
专利号:US-4965343-A 优先权日:1988-01-28 标题 :Method of peptide synthesis 发明人:FELIX ARTHUR M; FOURNIER ALAIN; DANHO WALEED 权利人:HOFFMANN LA ROCHE 摘要:A method for the solid phase synthesis of multi-sulfated peptides comprising coupling side-chain unprotected hydroxyamino acids to the peptide chain utilizing benzotriazol-1-yl-oxy-tris (dimethyl)-phosphonium hexafluorophosphate (BOP) as a coupling reagent.
专利号:US-8987504-B2 优先权日:2010-06-18 标题 :Aminohydroxylation of alkenes 发明人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL 权利人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL; VICTORIA LINK LTD 摘要:The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
[参考文献]: M J Lee, Et Al. Prodrugs Of Nitroxyl As Inhibitors Of Aldehyde Dehydrogenase. J Med Chem. 1992 Oct 2;35(20):3648-52. [参考文献]: Timothy A Wencewicz, Et Al. N-O Chemistry For Antibiotics: Discovery Of N-Alkyl-N-(Pyridin-2-Yl)Hydroxylamine Scaffolds As Selective Antibacterial Agents Using Nitroso Diels-Alder And Ene Chemistry. J Med Chem. 2011 Oct 13;54(19):6843-58.
合成参考文献
摘要:MacMillan, D. W. C.; Watson, A. J. B., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 371. 摘要:Liu, Y.; Melchiorre, P., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 419. 摘要:Casano, G.; Ouari, O., Science of Synthesis, (2021) , 47.