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71. 发明专利

JPH08157437A PRODUCTION OF D-AMINO ACID-N-(S)-ALPHA-ALKYLBENZYLAMIDE 失效
公开(公告)号：JPH08157437A
公开(公告)日：1996-06-18
申请号：JP30478394
申请日：1994-12-08
申请人： AJINOMOTO KK
发明人： TSUCHIYA TOYOHITO , MOCHIZUKI CHIAKI , TAKEMOTO TADASHI
IPC分类号： C07B53/00 , C07C231/12 , C07C231/16 , C07C237/06
摘要： PURPOSE: To inexpensively obtain the subject compound useful as a synthetic intermediate of a highly sweet material from an available raw material by racemizing a compound derived from a dehydrating condensation of L-amino acid-N-(S)-α-alkylbenzylamide with aryl aldehyde and hydrolyzing. CONSTITUTION: A compound expressed by formula I (C at * position has a L-amino acid structure; R1 is CH3 or C2 H5 ; X is H, a halogen, NO2 , CN, a lower alkyl or a lower alkoxy) derived from a dehydrating condensation reaction of L-amino acid-N-(S)-α-alkylbenzylamide with aryl aldehyde is brought into contact with a solvent (e.g. isopropanol) containing a racemization-accelerating base (e.g. diazabicycloundecene). In the solvent, an amino acid part of the compound is racemized to generate an N-substituted phenylmethylidene-D-amino acid-N-(S)-alkylbenzylamide and the resultant compound is hydrolyzed under an acidic condition, and aryl aldehyde is removed to obtain the object compound of the formula II (C at * position has a D-amino acid structure).

72. 发明专利

JPH0528697B2 失效
公开(公告)号：JPH0528697B2
公开(公告)日：1993-04-27
申请号：JP19968784
申请日：1984-09-26
申请人： HOECHST AG
发明人： ZUZANE GURAAPURAI
IPC分类号： C07B55/00 , B01J31/00 , B01J31/04 , C07B31/00 , C07B61/00 , C07C67/00 , C07C227/00 , C07C227/14 , C07C227/28 , C07C227/36 , C07C229/02 , C07C231/16 , C07C233/82 , C07C313/00 , C07C319/20 , C07C323/59 , C07F9/30 , C07F9/50

73. 发明专利

JPH0510333B2 失效
公开(公告)号：JPH0510333B2
公开(公告)日：1993-02-09
申请号：JP2721384
申请日：1984-02-17
申请人： SAGAMI CHEM RES
发明人： HYAMA TAMEJIRO , FUJITA MAKOTO
IPC分类号： C07C271/10 , C07C67/00 , C07C231/00 , C07C231/12 , C07C231/16 , C07C231/18 , C07C233/18 , C07C239/00 , C07C301/00 , C07C303/40 , C07C311/00

74. 发明专利

JPH041167A 1-ACEAMIDOINOSITOLS AND PRODUCTION THEREOF 失效
公开(公告)号：JPH041167A
公开(公告)日：1992-01-06
申请号：JP9980690
申请日：1990-04-16
申请人： YOKOHAMA RUBBER CO LTD
发明人： OGAWA SEIICHIRO , ISAKA AKIHIRO , KAGEYAMA KUNIO , MACHIDA MORIHISA
IPC分类号： C07C231/16 , C07C233/23
摘要： NEW MATERIAL:Optically active 1L-1-acetamido-3,4,5,6-tetra-O-acetyl-1-deoxy-2- O-methyl-chiro-inositol shown by formula l. USE:Useful as a starting substance for synthesizing aminocyclotols usable as a synthetic raw material for drugs such as antibiotics and anti-cancer drugs and agricultural chemicals. PREPARATION:A compound shown by formula I is obtained by using L- quebrachitol as a starting raw material, subjecting the 1-position thereof to azide formation, reducing the azide group and acetylating to give an acetylamino group and a process of converting the 3,4,5 and 6-orders of L-quebrachitol into Oacetyl groups. A compound shown by formula II is obtained by using L- quebrachitol as a starting raw material and the compound is also a new compound.

75. 发明专利

JPH0314014B2 失效
公开(公告)号：JPH0314014B2
公开(公告)日：1991-02-25
申请号：JP9926582
申请日：1982-06-11
申请人： BANYU PHARMA CO LTD
发明人： MATSUMOTO IKUO , ISHIKAWA KYOBUMI , YOSHIZAWA JUNJI
IPC分类号： C07C231/00 , C07C67/00 , C07C231/12 , C07C231/16 , C07C233/46 , C07C233/47

76. 发明专利

JPS61218564A IMPROVEMENT OF N-ACYL-ACYLOXY AROMATIC AMINE 失效
公开(公告)号：JPS61218564A
公开(公告)日：1986-09-29
申请号：JP5071986
申请日：1986-03-10
申请人： CELANESE CORP
发明人： SEODORUFU HORENKO , JIEEMUZU EICHI JIYOOJI
IPC分类号： C07B61/00 , B01J27/00 , B01J27/16 , B01J31/00 , B01J31/04 , C07C67/00 , C07C231/00 , C07C231/10 , C07C231/12 , C07C231/14 , C07C231/16 , C07C233/00 , C07C233/16 , C07C233/25 , C07C233/27

77. 发明专利

JPS5970654A Anthranilic acid derivative 失效
标题翻译：苯甲酸衍生物
公开(公告)号：JPS5970654A
公开(公告)日：1984-04-21
申请号：JP17997682
申请日：1982-10-15
申请人： Nippon Redarii Kk
发明人： SATOU TOSHIO , AOYANAGI SAKAE , KATOU ATSUYUKI
IPC分类号： C07C231/00 , A61K31/195 , A61K31/196 , A61P37/08 , C07C67/00 , C07C231/12 , C07C231/16 , C07C235/38
摘要： NEW MATERIAL:N-(cis-3,4-Dimethoxycinnamoyl)anthranilic acid expressed by formula I and a salt thereof.
USE: An antiallergic agent useful for treating bronchial asthma, urticaria, atopic dermatitis, allergic rhinitis, etc.
PROCESS: A solution of N-(trans-3,4-dimethoxycinnamoyl)anthranilic acid expressed by formula II or a salt thereof is irradiated with light containing ultraviolet rays having at least 310W315nm and/or 360W370nm, preferably 313nm and/ or 366nm, wavelength for at least 30min, preferably one hr or longer to give the aimed compound of formula I . A high pressure mercury lamp, medium pressure mercury lamp, etc. may be preferred for the irradiation light source, but direct rays of the sun, a fluorescent lamp or germicidal lamp, etc. may also be used.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：由式I表示的N-（顺式-3,4-二甲氧基肉桂酰基）邻氨基苯甲酸及其盐。用途：用于治疗支气管哮喘，荨麻疹，特应性皮炎，过敏性鼻炎等的抗过敏药物。方法：将由式II表示的N-（反式-3,4-二甲氧基肉桂酰）邻氨基苯甲酸或其盐的溶液照射包含具有至少310-315nm和/或360-370nm，优选313nm和/或366nm波长的紫外线至少30分钟，优选1小时或更长时间的紫外线的光，得到目标式I化合物。对于照射光源，优选高压汞灯，中压汞灯等，但也可以使用太阳，荧光灯，杀菌灯等的直接光线。

78. 发明专利

JPS58216147A Racemization of optical active n-acetyl-3-hydroxy- 4-(hydroxymethyl)phenylglycine 失效
标题翻译：光学活性N-乙酰基-3-羟基-4-（羟基甲基）苯甲酰胺的研究
公开(公告)号：JPS58216147A
公开(公告)日：1983-12-15
申请号：JP9926582
申请日：1982-06-11
申请人： Banyu Pharmaceut Co Ltd
发明人： MATSUMOTO IKUO , ISHIKAWA KIYOBUMI , YOSHIZAWA JIYUNJI
IPC分类号： C07C231/00 , C07C67/00 , C07C231/12 , C07C231/16 , C07C233/46 , C07C233/47
摘要： PURPOSE: To obtain the titled compound useful as an intermediate for synthesizing an immune activator, by heating optical active N-acetyl-3-hydroxy-4-(hydroxymethyl)phenylglycine in an aqueous solution of a specific amount of an alkali metal hydroxide.
CONSTITUTION: 1 equivalent optical active N-acetyl-3-hydroxy-4-(hydroxymethyl) phenylglycine is racemized in ≥2 equivalents, preferably 2W5 equivalents aqueous solution of alkali metal hydroxide at 40W100°C, to give the desired substance. ≥0.5 equivalent alkali metal acetate or boric acid is added to the reaction system during racemization to prevent acylation, and the concentration of the aqueous solution of alkali metal hydroxide is preferably 3W12 normalities.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：目的：通过在特定量的碱金属氢氧化物的水溶液中加热光学活性N-乙酰基-3-羟基-4-（羟甲基）苯基甘氨酸，得到可用作合成免疫激活剂的中间体的标题化合物。构成：在40-100℃，1当量光学活性N-乙酰基-3-羟基-4-（羟甲基）苯基甘氨酸在> = 2当量，优选2-5当量碱金属氢氧化物水溶液中外消旋，得到所需物质。 > = 0.5当量碱金属乙酸酯或硼酸在外消旋化反应体系中加入以防止酰化，碱金属氢氧化物水溶液的浓度优选为3-12标准。

79. 发明专利

JPS5835154A MANUFACTURE OF ALPHA-HALOALKYLAMIDES 失效
公开(公告)号：JPS5835154A
公开(公告)日：1983-03-01
申请号：JP895982
申请日：1982-01-25
申请人： STAUFFER CHEMICAL CO
发明人： RICHIYAADO DAGURASU GURESU JIY
IPC分类号： C07C231/02 , B01J27/00 , B01J27/08 , B01J27/125 , B01J27/135 , C01F7/48 , C01G23/02 , C01G25/04 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/16 , C07C233/02 , C07C233/05

80. 发明专利

JPS55355A PREPARATION OF *2S*3R* OR *2S*3S**33AMINOO22HYROXYPROPIONIC ACID DERIVATIVE 失效
公开(公告)号：JPS55355A
公开(公告)日：1980-01-05
申请号：JP2663279
申请日：1979-03-09
申请人： NIPPON KAYAKU KK
发明人： NISHIZAWA RINZOU , SAINO TETSUYUKI , SEYA KENJI
IPC分类号： C07C233/47 , C07C67/00 , C07C227/00 , C07C227/20 , C07C229/22 , C07C229/28 , C07C229/34 , C07C231/00 , C07C231/02 , C07C231/16 , C07C233/48 , C07C233/51 , C07C233/83
摘要： PURPOSE:Thionyl chloride is made to act on (2R,3R) isomer and (2R,3S) isomer, which are useless because they have no enzyme inhibition activity, and the hydrolysis is effected to produce title compound used for synthetic intermediate of immunologically activated carcinostatics. CONSTITUTION:Thionyl chloride or sulfonyl chloride is made to act on (2R,3R) or (2R,3S)-3-amino-2-hydroxypropionic ester derivative of the formula [R1 is cycloalkyl, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl; R2 is lower alkyl, phenyl, substituted phenyl; R3 is residue of ester] in such an amount that thionyl chlride or sulfonyl chloride can be used also as the solvent, 5-10 times equivalent at -10-10 deg.C. The resulting product is hydrolyzed with acid or alkali to produce the objective (2S,3R) or (2S,3S) isomer.

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