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91. 发明专利

JPS60163881A THIAZOLE DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS60163881A
公开(公告)日：1985-08-26
申请号：JP2065684
申请日：1984-02-06
申请人： KISSEI PHARMACEUTICAL
发明人： KOBAYASHI MICHIHIRO , KITAZAWA MAKIO , SAITOU TAKENAO
IPC分类号： C07D417/06 , A61K31/425 , A61K31/535 , A61P1/04 , C07D207/00 , C07D263/00 , C07D265/00 , C07D277/00
摘要： NEW MATERIAL:The compound of formula I (R is H or 1-3C alkyl; A is 1-4C alkylene; B is O; one of l and n is 1 and the other is 0 or 1: m is 1-3; sum of l, m and n is 3 or 4). EXAMPLE:3-[2-(4-Methyl-5-thiazolyl)ethyl]-2,4-oxazolidinedione. USE:Remedy and preventive for gastric and duodenal ulcer of mammals including man. PREPARATION:The compound of formula I can be produced by reacting the omega- haloalkylthiazole derivative of formula II (X is Cl, Br or I) with the compound of formula III and it alkali metal salt in the presence or absence of a basic substance (e.g. K2CO3).

92. 发明专利

JPS60155173A NOVEL BETA-HYDROXY ESTER 失效
公开(公告)号：JPS60155173A
公开(公告)日：1985-08-15
申请号：JP16440984
申请日：1984-08-06
申请人： RIKAGAKU KENKYUSHO
发明人： OOISHI TAKESHI , HORIKOSHI KOUKI , AKITA HIROYUKI , KOSHIJI HIROKO , FURUICHI AKINARI
IPC分类号： C07D307/54 , C07D209/00 , C07D263/00 , C07D413/04 , C07D413/06 , C12P17/04 , C12P41/00 , C12R1/645 , C12R1/72 , C12R1/725 , C12R1/74 , C12R1/78 , C12R1/84 , C12R1/85 , C12R1/865 , C12R1/88
摘要： NEW MATERIAL:The beta-hydroxy ester of formula I (X is alpha- or beta-CH3; Y is alpha- or beta-OH). EXAMPLE:The compound of formula II. USE:A synthetic intermediate of indolmycin of formula III effective to staphylococci resistant to various commercial antibiotic substances separated from Streptomyces albus, etc. PREPARATION:The condensation reaction of the aldehyde of formula III with the alpha-haloester of formula IV (X is halogen) in the presence of Zn affords the optical isomer of the beta-hydroxy ester of formula V, which is made to react with an oxidizing agent to obtain the starting substance of formula VI. Microbial strain of e.g. Candida genus, or its cell is inoculated and cultured in a medium containing the starting substance. The cultured product is filtered with celite, etc., and the filtrate is extracted with an organic solvent and dried. The obtained crude compound of formula I is purified by direct silica gel column chromatography to obtain the optically active compound of formula I having high optical purity in high yield.

93. 发明专利

JPS6028966A PREPARATION OF ACYLMETHYLENE DERIVATIVE OF N-SUBSTITUTED HETEROCYCLIC COMPOUND 失效
公开(公告)号：JPS6028966A
公开(公告)日：1985-02-14
申请号：JP12750483
申请日：1983-07-12
申请人： MITSUBISHI PAPER MILLS LTD
发明人： ITOU AKIRA
IPC分类号： C07D235/12 , C07D263/00 , C07D263/56 , C07D277/64 , C07D307/00 , C07D333/00 , C07D413/06 , C07D487/04 , C07D498/04
摘要： PURPOSE:To obtain the titled substance useful as an intermediate for the synthesis of cyanine dye, under mild condition in high yield, by condensing 2-ethylaminophenol, etc. with 3,3-dichloroacrylophenone, etc. CONSTITUTION:The objective compound of formula III is prepared by reacting (A) the compound of formula I [D is (substituted) arylene or bivalent heterocyclic group; R is (substituted) alkyl or aralkyl; Q is O, S or NR (R is alkyl, aralkyl, etc.)] with (B) the compound of formula II [R is (substituted) alkyl, aralkyl, aryl or heterocyclic group; X is halogen, lower alkoxy or mercapto] preferably in 1,4-dioxane in the presence of a base such as triethylamine at a temperature between room temperature and the boiling point of the solvent. The compound of formula III wherein Q is O or NR is novel substance.

94. 发明专利

JPS59216882A Production of 2,4-oxazolidinedione derivative 失效
标题翻译： 2,4-二氧杂环己烷衍生物的制备
公开(公告)号：JPS59216882A
公开(公告)日：1984-12-06
申请号：JP8979783
申请日：1983-05-20
申请人： Kissei Pharmaceut Co Ltd
发明人： KOBAYASHI MICHIHIRO , KITAZAWA MAKIO , SAITOU TAKENAO
IPC分类号： C07D263/44 , C07D263/00 , C07D333/00 , C07D413/04 , C07D413/06
摘要： PURPOSE: To obtain the titled substance useful as a synthetic intermediate for medicines safely in constant yield, by reacting a 2-hydroxycarboxylic acid ester with an alkali cyanide in a polar organic solvent, and treating the reaction product if necessary with an acid.
CONSTITUTION: A compound of formula I (R
1 is H, lower alkyl, aryl, aralkyl or heterocyclic ring group; R
2 is H or lower alkyl; R
3 is lower alkyl) is reacted with an alkali cyanide in a polar organic solvent, e.g. 1-butanol, at 100W150°C for 10W30hr, and the reaction product is if necessary treated with an acid to give the aimed compound of formula II (M is alkali metal).
EFFECT: The aimed substance in a large amount can be obtained in constant yield using the safe and stable alkali cyanide.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：通过使2-羟基羧酸酯与碱金属氰化物在极性有机溶剂中反应，以稳定的产率获得用作药物的合成中间体的标题物质，并根据需要用酸处理反应产物。构成：式Ⅰ化合物（R 1为H，低级烷基，芳基，芳烷基或杂环基; R 2为H或低级烷基; R 3为低级烷基）与碱金属氰化物在极性有机溶剂中反应。 1-丁醇，在100-150℃下反应10-30小时，如果需要用酸处理反应产物，得到目标化学式II（M是碱金属）。效果：使用安全稳定的碱性氰化物可以以恒定的产率获得大量的目标物质。

95. 发明专利

JPS5921681A 1-sulf-2-oxo-azetidine derivative and manufacture 失效
标题翻译： 1-SULF-2-OXO-AZETIDINE衍生和制造
公开(公告)号：JPS5921681A
公开(公告)日：1984-02-03
申请号：JP9815183
申请日：1983-06-03
申请人： Hoffmann La Roche
发明人： ANDORE FURURENMAIYAA , BERUNAA HOOFUHAINTSU , KURISUCHIYAN NIKORA HIYUBUSHIY , HANSU PEETAA IIZENRINKU
IPC分类号： C07D401/12 , A61K20060101 , A61K31/397 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/433 , A61P31/04 , B01J23/44 , B01J27/13 , B01J27/16 , C07B61/00 , C07D20060101 , C07D205/08 , C07D205/085 , C07D213/55 , C07D213/73 , C07D231/12 , C07D233/88 , C07D263/00 , C07D263/48 , C07D277/00 , C07D277/20 , C07D277/40 , C07D277/74 , C07D285/08 , C07D403/12 , C07D413/12 , C07D417/12 , C07D419/12 , C07D521/00 , C07F7/18
CPC分类号： Y02P20/52
摘要： Title compds. I [Het=aromatic heterocycle R1=H, alkyl, alkanoyl, R2=H, alkenyl, are prepd. Thus, 2-[5-(1-tertiany -butoxyformamide)- 3-(1,2,4-thiacliazolyl) -2-[[(Z)-(tertiarybutoxycarbonyl) methoxyl imino!acetate 2-benzthiazollyl thio ester is treated with 1- chloro-N, N, 2-trimethyl-1-propenamine, triethyl amine, and (3S,4S)- 3-amino-4-carbamoyloxymethyl)-2-oxo-1-azetidine sulfonate. After stirring and evaporating, the resulting residue is reacted with NaHCO3 to give (3S,4S)-3-[(Z)-2-(5-amino-1,2,4thiadiazol-3-yl)-2- [[(t-butoxycarbonyl)methoxy imino!acetamido!4-carbamoyloxymethyl-2- oxo-1-azetidine sulfonate.

96. 发明专利

JPS59500054A JPS59500054A - 失效
公开(公告)号：JPS59500054A
公开(公告)日：1984-01-12
申请号：JP50031782
申请日：1982-01-22
IPC分类号： C07D213/00 , A61K31/44 , C07D20060101 , C07D213/50 , C07D213/53 , C07D263/00 , C07D413/00 , C07D413/04

98. 发明专利

JPS58134083A NOVEL 1,4-BIS(SUBSTITUTED AMINO)-5,8- DIHYDROXYANTHRAQUINONES, MANUFACTURE AND MEDICINE 失效
公开(公告)号：JPS58134083A
公开(公告)日：1983-08-10
申请号：JP1384583
申请日：1983-02-01
申请人： AMERICAN CYANAMID CO
发明人： KEISU CHIYADOUITSUKU MAADOTSUK
IPC分类号： C09K3/00 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/44 , A61P35/00 , C07D263/00 , C07D263/04 , C07D263/06 , C07D263/16 , C07D263/52 , C07D265/32 , C07D267/10 , C07D413/14

99. 发明专利

JPS5855482A NOVEL 2,3-DIHYDRO-1,4-BENZODIOXINE DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS5855482A
公开(公告)日：1983-04-01
申请号：JP15230181
申请日：1981-09-26
申请人： KYOWA HAKKO KOGYO KK
发明人： TERANISHI MASAYUKI , OBASE HIROYUKI , TAKAI HARUKI , NOMOTO YUUJI , SHIYUTOU SHIYOUICHI , KARASAWA HIROSHI , KASUYA YUTAKA
IPC分类号： C07D413/14 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/54 , A61P9/12 , A61P29/00 , C07D211/00 , C07D233/00 , C07D239/00 , C07D249/00 , C07D263/00 , C07D285/00 , C07D319/00 , C07D405/14 , C07D417/14
摘要： NEW MATERIAL:The compound of formulaI[Q is CO or CH(OR); R is H or acyl; X is heterocyclic group of formula II, formula III, etc.; R1 is H or acyl], and its pharmacologically permissible acid addition salt. EXAMPLE:2-{2-[4-(2-Oxo-3,4-dihydro-2H-1,3-benzoxazin-3-yl)piperidin-1- yl]-oxoethyl}-2,3-dihydro-1,4-benzodioxine. USE:An antihypertension and antiphlogistic agent. It exhibits excellent pharmacological activity, and is useful as a medicine. PROCESS:The compound of e.g. formula VI can be prepared by reacting the compound of formula IV with an optically active novel compound of formula V (Z is halogen or eliminable group) in an inert solvent such as acetone, chloroform, DMF, etc.

100. 发明专利

JPS5632306B1 失效
公开(公告)号：JPS5632306B1
公开(公告)日：1981-07-27
申请号：JP4615871
申请日：1971-06-24
IPC分类号： A61K31/395 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/47 , C07D205/00 , C07D205/08 , C07D215/00 , C07D263/00 , C07D277/00 , C07D401/12 , C07D413/12 , C07D417/12

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