CAS: 32981-85-4; Bz-Rs-Iser(3-Ph)-Ome

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CAS号98-88-4 苯甲酰氯 | CAS号145041-37-8 methyl (2R,3S)-... | CAS号186581-53-3 重氮甲烷 | CAS号132201-33-3 N-苯甲酰基-(2R,3S)-... | CAS号67-56-1 甲醇 | CAS号100-44-7 氯化苄 | CAS号33069-62-4 紫杉醇 | CAS号32981-85-4 (2R,3S)-3-苯甲酰氨基... | CAS号132201-33-3 N-苯甲酰基-(2R,3S)-... | CAS号136561-53-0 (2R,3S)-3-苯基异丝胺酸 | CAS号153652-70-1 (4S,5R)-3-苯甲酰基-...

Methyl Cinnamate置于lipase Ps-C M. Miehei,Sodium Hydride,Caesium Carbonate,Magnesium Bromide Ethyl Etherate体系中,用 四氢呋喃,乙醚,正己烷,二氯甲烷,Mineral Oil 作为反应溶剂,化学反应 116.0H,反应生成 N-苯甲酰基-(2R,3S)-3-苯基异丝氨酸甲酯
参考文献:Regio-And Stereoselective Methods For The Conversion Of (2S,3R)-β-Phenylglycidic Acid Esters To Taxoids And Other Enantiopure (2R,3S)-Phenylisoserine Esters
标题:Regio-And Stereoselective Methods For The Conversion Of (2S,3R)-β-Phenylglycidic Acid Esters To Taxoids And Other Enantiopure (2R,3S)-Phenylisoserine Esters
摘要:提出了一种新的高效方法,用于合成含类固醇的对映体前体,即 (2R,3S)-和 (2S,3R)-N-苯甲酰基苯基异丝氨酸的甲酯以及类似的类固醇酯.该方法基于对相应的反式-β-苯基甘氨酸对映体进行区域和立体选择性氢溴酸分解,对得到的 3-溴烷烃进行 O-酰基氨基甲酰化的连续反应,分子内环化为 4-苯基恶唑啉-2-酮-5-羧酸衍生物,以及恶唑啉酮开环.
DOI:10.1007/s11172-012-0302-4

专利信息

专利号:US-6020174-A
优先权日:1992-07-27
标题:Chemoenzymatic synthesis of the taxol C-13 side chain N-benzolyl- (2R,3S)-Phenylisoserine
发明人：CHEN CHING-SHIH; GOU DA-MING; LIU YEUK-CHUEN
权利人:RHODE ISLAND EDUCATION
摘要:(2R,3S)- and (2S,3R)-enantiomers of trans- beta -phenylglycidic esters, prepared by lipase-mediated enantioselective transesterification, are used for the synthesis of the taxol C-13 side chain with good yield.

专利号:US-6509506-B1
优先权日:1997-05-21
标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino aldehydes
发明人：SHARPLESS K BARRY; LI GUIGEN
权利人:SCRIPPS RESEARCH INST
摘要:D- and L- α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydoxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- α-amino acid or D- and L-α-amino aldehyde.

专利号:US-5994583-A
优先权日:1996-05-22
标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino-aldehydes
发明人：SHARPLESS K BARRY; LI GUIGEN
权利人:SCRIPPS RESEARCH INST
摘要:D- and L-α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydroxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L-α-amino acid or D- and L-α-amino aldehyde.

专利号:WO-9310076-A1
优先权日:1991-11-22
标 题 :Synthesis and optical resolution of the taxol side chain and related compounds
发明人：PETERSON JOHN R; ZJAWIONY JORDAN K; ROGERS ROBIN D
权利人:UNIV MISSISSIPPI
摘要:This invention relates to a method for the production of a substantially optically pure taxane side chain comprising the steps of synthesizing a racemic mixture of enantiomers of the taxane side chain that is capable of exhibiting conglomerate behavior and resolving the substantially optically pure enantiomers by direct crystallization methods. This invention also relates to the semisynthesis of taxanes such as taxol through coupling the substantially optically pure taxane side chain to a taxane ring nucleus.

专利号:US-5932758-A
优先权日:1995-07-04
标 题 :Process for the production β-amino-α-hydroxycarboxylic acids and derivatives thereof
发明人：STINGL KLAUS; KOTTENHAHN MATTHIAS; DRAUZ KARLHEINZ
权利人:DEGUSSA
摘要:Disclosed is a process for producing β-amino-α-hydroxycarboxylic acid derivatives of general formula (2R,3S)- or (2S,3E)-N-(X,Y)-3-amino-2-hydroxy-3-phenyl propionic acid-Z of Formula I, ##STR1## e.g. of (2E,3S)-3-amino-2-hydroxy-3-phenyl propionic acid or (2R,3S)-N-benzoyl-3-amino-2-hydroxy-3-phenyl propionic acid methylester. Compounds of type I are valuable intermediates in the total synthesis of Taxols which can be used in the treatment of various forms of cancer.

专利号:WO-9744312-A1
优先权日:1996-05-22
标题:TWO STEP SYNTHESIS OF D- AND L- α-AMINO ACIDS AND D- AND L- α-AMINO ALDEHYDES