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81. 发明专利

JPS61189253A HOMOTYROSINE DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPS61189253A
公开(公告)日：1986-08-22
申请号：JP2773885
申请日：1985-02-15
申请人： SUNTORY LTD
发明人： OOFUNA YASUSHI , KUROKAWA NATSUKO
IPC分类号： C07C227/02 , C07C67/00 , C07C227/00 , C07C227/20 , C07C229/36
摘要： NEW MATERIAL:A compound shown by the formula I. EXAMPLE:( 2R,3R ) - 4 - ( 4 - t - B u tyldimethylsilyloxyphenyl)-3-(2-tetrahydropyranyl)oxy-2-N-t-butoxycarb onylamino-butyl-2-acetate. USE:Useful as an antifungal agent especially a drug such as an anti-yeast, anti-mold, etc., an animal drug, or a drug for central nervous system. PREPARATION:A 4-phenylbutylacylate shown by the formula II (R -R are protecting group; R is acyl) is hydrolyzed by the use of a base (e.g., Na2CO3, K2CO3, etc.), then oxidized, deprotected with a weak acid, to give a homotyrosine derivative shown by the formula I. When an optically active compound is used as a starting raw material in the reaction, the reaction is advanced sterically selectively, the aimed compound is obtained as an optically active substance and when an optically inactive substance is used, the aimed compound is obtained as an optically inactive substance.

82. 发明专利

JPS617184B2 JPS617184B2 - 失效
公开(公告)号：JPS617184B2
公开(公告)日：1986-03-04
申请号：JP654678
申请日：1978-01-24
申请人： Ajinomoto Kk
发明人： AJISAKA KATSUMI , PPONMA MASAO
IPC分类号： C11D1/88 , A61K8/00 , A61K8/30 , A61K8/37 , A61K8/44 , A61Q5/00 , A61Q5/02 , A61Q7/00 , A61Q17/00 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/20 , C07C229/24 , C09K3/00 , C11D1/90
CPC分类号： Y02P20/55

83. 发明专利

JPS6133149A Preparation of cyclopropylglycine derivative 失效
标题翻译：环丙基胆碱衍生物的制备
公开(公告)号：JPS6133149A
公开(公告)日：1986-02-17
申请号：JP15449984
申请日：1984-07-25
申请人： Suntory Ltd
发明人： OOFUNA YASUSHI , KUROKAWA NATSUKO
IPC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
CPC分类号： Y02P20/55
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 CH
2 N
2 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).
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过在金属催化剂的存在下水解2-氨基-3-戊烯酸酯衍生物作为原料，容易且有效地获得具有新骨架的标题化合物，可用于农药等，构成：由式I表示的2-氨基-3-戊烯酸衍生物（R 3是低级酰氧基; R 4是氨基的保护基; R 5是低级烷基或芳烷基）在金属催化剂，优选氯化钯 - 二乙腈络合物等的存在下与式CH 2 N 2表示的重氮甲烷反应，得到式II表示的目的化合物（R为低级酰氧基甲基; R 1为保护基的氨基; R 2是R 5）。然后将由式II表示的所得化合物用> = 2当量碱水解，得到由式II表示的目标化合物（R为羟甲基; R 1为氨基的保护基; R 2为H）。然后用弱酸等除去保护基，或用氧化剂氧化，进一步水解，得到由式II表示的目标化合物（R为羧基; R 1和R 2为H）。

84. 发明专利

JPS60233041A NOVEL LYSINE ESTERS USEFUL AS ABSORPTION ENHANCER 失效
公开(公告)号：JPS60233041A
公开(公告)日：1985-11-19
申请号：JP8912385
申请日：1985-04-26
申请人： MERCK & CO INC
发明人： JIYOSEFU EE FUIKUSU , SUTEFUANO EE POGANII
IPC分类号： A61K47/16 , A61K9/00 , A61K31/12 , A61K31/22 , A61K47/18 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/20 , C07C229/26

90. 发明专利

JPS6023354A MANUFACTURE OF PURE L-LEUCINE 失效
公开(公告)号：JPS6023354A
公开(公告)日：1985-02-05
申请号：JP10188184
申请日：1984-05-22
申请人： DEGUSSA
发明人： AKUSERU KUREEMAN , YURUGEN MARUTENSU , HORUSUTO BUAIGERU
IPC分类号： C12P13/06 , C07C67/00 , C07C227/00 , C07C227/20 , C07C227/28 , C07C227/40 , C07C229/08

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