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.
专利号:US-5530124-A 优先权日:1994-06-30 标 题:Method for preparing cyclic ureas and their use for the synthesis of HIV protease inhibitors 发明人:RADESCA LILIAN A; HARRIS GREGORY D; WAT EDWARD K W; WALTERMIRE ROBERT E 权利人:DU PONT MERCK PHARMA 摘要:This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.
专利号:US-5744611-A 优先权日:1994-09-03 标题 :Process for the reduction of amino acids and the derivatives thereof 发明人:KOTTENHAHN MATTHIAS; DRAUZ KARLHEINZ; HILPERT HANS 权利人:DEGUSSA; HOFFMANN LA ROCHE 摘要:A process is disclosed for reducing amino acids and derivatives thereof Compounds of formula (I), in which n=0 or 1 and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meanings given in the description, are reduced to the corresponding amino alcohols of formula (II): the formula (I) compounds are converted in a first step, in at least one alcohol and with the addition of acid and heat to an ester, this process producing a reaction mixture containing the ester; the ester is converted in a second reaction step with alkali or alkaline earth borohydride to compounds of formula II. By specifying that the second step be carried out without isolating the ester from the reaction mixture and by using alkali or alkaline earth borohydrides which are not activated, the invention facilitates the production from amino acids and their derivatives of the correponding alcohols in a simple 'single vessel' process, with high yields and in such a way as to preserve a given centre of chirality. Applications: synthesis components, preparation of optically active compounds splitting of racemic compounds. ##STR1##
专利号:US-5322963-A 优先权日:1991-02-05 标 题 :Method for preparing α-amino-β, δ-diol derivatives 发明人:SHIBATA SAIZO; SHIRAKAWA EIJI; YAMADA YASUKI; ANDO KOJI; UCHIDA ITSUO 权利人:JAPAN TOBACCO INC 摘要:Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of α-amino aldehyde derivative [I] and compound [II] in the presence of BF 3 .OEt 2 , as shown in the following reaction formula, α-amino-β-hydroxy-δ-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R 1 is a protective group on the amino group, R 2 is a lower alkyl group which may be branched, and R 4 is a cyclohexyl group or phenyl group).
参考标题:An Expedient Route For The Reduction Of Carboxylic Acids To Alcohols Employing 1-Propanephosphonic Acid Cyclic Anhydride As Acid Activator 作者:G. Nagendra,C. Madhu,T.M. Vishwanatha,Vommina V. Sureshbabu |发布日期:2012.9 摘要:Method For The Synthesis Of Alcohols From The Corresponding Carboxylic Acids Is Described. Activation Of Carboxylic Acid With 1-Propanephosphonic Acid Cyclic Anhydride (T3P) And Subsequent Reduction Using Nabh4 Yield The Alcohol In Excellent Yields With Good Purity. Reduction Of Several Alkyl/aryl Carboxylic Acids And Nα-Protected Amino Acids/peptide Acids As Well As Nβ-Protected Amino Acids Was Successfully