发明名称 PREPARATION OF CYCLOPROPYLGLYCINE DERIVATIVE
摘要 PURPOSE:To obtain easily and efficiently the titled compound, having a new skeleton, and useful for agricultural chemicals, etc., by hydrolyzing a 2-amino-3- pentenoic acid ester derivative as a raw material in the presence of a metal catalyst, etc. CONSTITUTION:A 2-amino-3-pentenoic acid derivative expressed by formula I (R<3> is lower acyloxy; R<4> is a protecting group of the amino group; R<5> is lower alkyl or aralkyl) is reacted with a diazomethane expressed by the formula CH2N2 in the presence of a metal catalyst, preferably palladium chloride-diacetonitrile complex, etc. to afford the aimed compound expressed by formula II (R is lower acyloxymethyl; R<1> is a protecting group of the amino group; R<2> is R<5>). The resultant compound expressed by formula II is then hydrolyzed with >=2 equivalents base to give the aimed compound expressed by formula II (R is hydroxymethyl; R<1> is a protecting group of the amino group; R<2> is H). The protecting group is then removed with a weak acid, etc. or oxidized with an oxidizing agent and further hydrolyzed to afford the aimed compound expressed by formula II (R is carboxyl; R<1> and R<2> are H).
申请公布号 JPS6133149(A) 申请公布日期 1986.02.17
申请号 JP19840154499 申请日期 1984.07.25
申请人 SUNTORY LTD 发明人 OOFUNA YASUSHI;KUROKAWA NATSUKO
分类号 C07B61/00;B01J23/00;B01J23/72;B01J27/00;B01J27/13;B01J31/00;B01J31/04;B01J31/12;B01J31/22;B01J31/24;C07C67/00;C07C227/00;C07C227/16;C07C227/18;C07C227/20;C07C229/28;C07C229/46 主分类号 C07B61/00
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