-
公开(公告)号：JPS61112067A
公开(公告)日：1986-05-30
申请号：JP24681885
申请日：1985-11-01
IPC分类号： C07D311/30
摘要： PURPOSE: To produce the titled compound useful as a remedy for cystectasy or vesical hypersensitivity, etc., in high purity and yield, in short steps, by dehalogenating the novel 6-halogeno-3-methylflavone-8-carboxylic acid.
CONSTITUTION: The objective compound of formula III is prepared economically in an industrial scale, by reacting the novel substance of formula I [R is H, lower alkyl or group of formula II (R
1 and R
2 are lower alkyl or R
1 and R
2 are bonded together with a hetero atom to form a heterocyclic group together with the N atom bonded thereto; n is integer of 1W4); X is halogen], in a proper solvent in the presence of a conventional dehalogenation catalyst and preferably a fatty acid alkali metal salt. The novel substance of formula I used as the starting material can be produced by preparing the novel substance of formula VI from the compound of formula IV via the compound of formula V, and heating the compound of formula VI together with an alkali metal benzoate and benzoyl halide or benzoic anhydride.
COPYRIGHT: (C)1986,JPO&Japio摘要翻译： 目的：通过使新型6-卤代-3-甲基黄酮-8-羧酸脱卤，制备标题化合物，可用于高胆固醇或血浆超敏反应的补救方法，以高纯度和产率。 结构式：式III的目标化合物是经济地制备的，通过使式I [R是H，低级烷基或式II基团（R 1和R 2）是低级烷基或 R 1和R 2与杂原子键合在一起，与与其结合的N原子一起形成杂环基; n为1-4的整数）; X是卤素]，在常规脱卤催化剂存在下，在适当的溶剂中，优选为脂肪酸碱金属盐。 用作起始原料的式I的新物质可以通过式V化合物通过式V化合物制备式VI的新物质，并将式VI化合物与碱金属苯甲酸酯和苯甲酰基 卤化物或苯甲酸酐。
-
公开(公告)号：JPS5967281A
公开(公告)日：1984-04-16
申请号：JP17130382
申请日：1982-09-30
IPC分类号： A61K31/35 , A61K31/352 , A61P9/08 , A61P9/10 , C07D295/088 , C07D311/30
CPC分类号： C07D295/088 , C07D311/30
摘要： NEW MATERIAL:A compound shown by the formula [R is H, lower alkyl, or group shown by the formula I (R
1 and R
2 are lower alkyl, or R
1 and R
2 together with N to which they are linked may be bonded to form hetero ring; n is 1W4); X is halogen].
EXAMPLE: 3-Methylflavone-8-carbvoxylic acid methyl ester.
USE: Useful as an intermediate for synthesizing 3-methyl-flavone-8-carboxylic acid derivative useful as a remedy for elimination of subjective symptom of pollyakiuria and residual urine, having a vasodilating action on coronary artery, useful for preventing attack of angina pectoris, myocardial infarction, etc.
PROCESS: A 3-propionylsalicylic acid derivative shown by the formula III is heated with an alkali metal benzoate and a benzoyl halide or benzoic anhydride usually at about 150W200°C, to give a compound shown by the formula I . A compound shown by the formula III of a raw material is a novel compound.
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新材料：式[R为H，低级烷基或式I所示的基团（R 1和R 2）为低级烷基，或R 1和R 2与 它们所连接的N可以键合形成杂环; n为1-4）; X为卤素]。 实施例：3-甲基黄酮-8-甲酯酸甲酯。 用途：可用作合成3-甲基黄酮-8-羧酸衍生物的中间体，其用作消除肺炎和残余尿的主观症状的补救措施，对冠状动脉具有血管扩张作用，可用于预防心绞痛发作， 心肌梗塞等。方法：将式III所示的3-丙酰水杨酸衍生物与碱金属苯甲酸酯和苯甲酰卤或苯甲酸酐通常在约150-200℃加热，得到式 一世 。 原料化学式Ⅲ所示的化合物是新化合物。
-
公开(公告)号：JPS5967242A
公开(公告)日：1984-04-16
申请号：JP17130482
申请日：1982-09-30
IPC分类号： C07C67/00 , C07C51/00 , C07C51/353 , C07C51/373 , C07C65/40 , C07C69/84 , C07C69/88 , C07C213/00 , C07C219/12 , C07D205/08 , C07D295/08 , C07D295/088 , C07D311/30
CPC分类号： C07D295/088 , C07C51/373 , C07C65/40 , C07D311/30 , Y10S514/869 , Y10S514/929
摘要： NEW MATERIAL:A 3-propionylsalicyclic acid derivative of formula I [R is H, lower alkyl or formula II (R
1 and R
2 are lower alkyl or R
1 and R
2 together with the nitrogen atom to which they are linked through or not through a hetero atom may form a heterocyclic ring; n is an integer 1W4); X is H or halogen, provided that R represents formula II when X is H atom].
EXAMPLE: Ethyl-5-chloro-3-propionylsalicylate.
USE: Useful as a remedy for preventing the fit of angina pectoris and cardiac infraction, etc. and a remedy for increasing the discharge capacity of the urinary bladder, disappearance of subjective symptom of thamuria, etc. having coronary arterial vasodilator action and coronary blood stream increasing action, and further useful as a synthetic intermediate for compounds useful as a diuretic having the remissive action, e.g. smooth muscle spasm in the lower urinary tract.
PROCESS: A compound of formula III (X' is halogen) is reacted with a propionyl halide by the Friedel-Crafts reaction to give the aimed compound of formula I .
COPYRIGHT: (C)1984,JPO&Japio摘要翻译： 新材料：式I的3-丙酰基水杨酸衍生物[R是H，低级烷基或式II（R 1和R 2）是低级烷基或R 1和R 2与氮原子一起 它们通过或不与杂原子连接在一起可以形成杂环; n是整数1-4）; X是H或卤素，条件是当X是H原子时，R表示式II）。 实施例：乙基-5-氯-3- propionylsalicylate。 用途：可用作预防心绞痛和心脏梗死等适应症的补救措施，以及增加膀胱排出能力的补救措施，具有冠状动脉血管扩张作用和冠状动脉血流的饱腹感主要症状消失 增加作用，并且还可用作用作具有缓和作用的利尿剂的化合物的合成中间体，例如 下尿路平滑肌痉挛。 方法：通过Friedel-Crafts反应将式III化合物（X'是卤素）与丙酰卤反应，得到目标化合物I。
-
公开(公告)号：JPS57118562A
公开(公告)日：1982-07-23
申请号：JP476581
申请日：1981-01-13
IPC分类号： C07D209/43 , C07D209/08
摘要： PURPOSE: To obtain the titled compound as a β-sympatholytic agent simply in high purity and in high yield, by reacting an epoxy compound such as glucidopropylamide, etc. as a raw mateial with 4-hydroxyinodole, followed by reducing the reaction product.
CONSTITUTION: An epoxy compound (e.g., glycidamide, etc.) shown by the formulaI(R is H or lower alkyl) as a raw mateial is reacted with 4-hydroxyindole shown by the formula II, to give a 4-hydroxyindole derivative shown by the formula III, which is reduced, to give a 4-hydroxyindole derivative shown by the formula IV. The reduction, for example, is carried out in the presence of a catalyst such as lithium aluminum hydride, etc. The first reaction is done at normal temperature W60°C, preferably at 30W50°C, and the reduction is carried out at 0W50°C, preferably 10W30°C.
COPYRIGHT: (C)1982,JPO&Japio摘要翻译： 目的：通过使具有4-羟基吲哚的原料中的环氧化合物如葡聚糖丙二酰胺等与高纯度，高产率的β-交替溶解剂一起获得标题化合物，然后还原反应产物。 构成：由式I（R为H或低级烷基）作为原料的环氧化合物（如缩水甘油酰胺等）与式II所示的4-羟基吲哚反应，得到4-羟基吲哚衍生物， 将式III还原，得到式IV所示的4-羟基吲哚衍生物。 还原反应例如在氢化锂铝等催化剂存在下进行。第一反应在常温-60℃，优选30-50℃进行，还原反应 在0-50℃，优选10-30℃进行。
-
公开(公告)号：JPS56115771A
公开(公告)日：1981-09-11
申请号：JP2100680
申请日：1980-02-20
IPC分类号： C07D209/43 , C07D209/08
摘要： PURPOSE:To obtain the titled high-purity compound which is an intermediate for a dye, etc. in improved yield and through easy purification steps, by hydrogenating a novel nitrobenzene derivative, e.g. a readily preparable 6-methoxy-2-nitrobenzyl cyanide, as a raw material. CONSTITUTION:A novel nitrobenzene derivative, e.g. 6-ethoxy-2-nitrobenzyl cyanide or 6-n-propoxy-2-nitrobenzyl cyanide, expressed by formula I (R is alkyl) as a raw material is hydrogenated, or further the resultant 4-oxo-4,5,6,7-tetrahydroindole is heat-treated or hydrogenated to give a 4-alkoxyindole of formula II, which is then reacted with a hydrogen halide to afford 4-hydroxyindole. The compound of formula I is prepared from m-nitrophenol as a starting material readily.
-
公开(公告)号：JPS6393748A
公开(公告)日：1988-04-25
申请号：JP24013586
申请日：1986-10-08
IPC分类号： C07C69/612 , C07C69/65
摘要： PURPOSE:To advantageously obtain the titled substance which is an antipyretic agent, by reacting a readily available and inexpensive alkyl lactate tosylate as a starting material with benzene and then a monohalogenomethyl ether and metal chloride and reacting the resultant novel product with a Grignard reagent. CONSTITUTION:An alkyl lactate tosylate expressed by formula I (R is lower alkyl) is reacted with benzene in a solvent in the presence of a Lewis acid, normally at 0-70 deg.C. The resultant compound expressed by formula II is then reacted with a monohalogenomethyl ether expressed by formula III (X is halogen) and metal chloride, e.g. stannic chloride, etc., in a solvent at 0-30 deg.C to provide a 2-(4-halogenomethylphenyl)propionic acid ester expressed by formula IV which is a novel compound. The resultant novel compound expressed by formula IV is subsequently reacted with a Grignard reagent expressed by formula V to give a compound expressed by formula VI, which is then hydrolyzed to afford the aimed compound expressed by formula VII.
-
公开(公告)号：JPH0269473A
公开(公告)日：1990-03-08
申请号：JP22214788
申请日：1988-09-05
发明人： YAMAMOTO KEIKI , NISHIGUCHI IKUZO , TSUEMURA YOSHIHARU , INOUE HIROSHIGE , MIZUNO TAKUMI , HIRASHIMA TSUNESUKE
IPC分类号： C07D333/24 , A61K31/38 , A61K31/381 , A61P25/04 , A61P29/00
摘要： PURPOSE:To obtain the subject substance from an inexpensive raw material under mold condition in high purity and yield by reacting an (alkyl)thiophene with an acid halide and reacting the reaction product with orthoformates in the presence of an active iodine source. CONSTITUTION:The objective compound of formula IV can be produced by reacting a compound of formula I (R is H or alkyl) with a compound of formula II (R is H or alkyl; X is halogen) at -5-+20 deg.C using AlCl3, etc., as a catalyst and reacting the reaction product of formula III with 1-14 times weight of an orthoformate in the presence of an active iodine source (e.g., iodine or methyl iodide) at 10-30 deg.C. The reaction rate of the above reaction can be increased by the addition of a protonic acid or Lewis acid. The active iodine source and the orthoformates can be recovered in high yield without using a precision apparatus. The compound of formula IV is useful as an intermediate for analgesic and anti-inflammatory agent.
-
公开(公告)号：JPH01175958A
公开(公告)日：1989-07-12
申请号：JP33247487
申请日：1987-12-28
IPC分类号： C07B61/00 , B01J27/125 , B01J27/135 , C07C67/30 , C07C67/313 , C07C67/343 , C07C69/92
摘要： PURPOSE:To obtain a compound useful as a synthetic intermediate for drugs in high purity and in high yield, by reacting a salicyclic acid derivative with a tertiary butyl compound/isobutylene in the presence of Friedel-Craft catalyst and reacting the resulting substance with a propionyl halide. CONSTITUTION:A salicylic acid derivative shown by formula I [R is H, lower alkyl or -(CH2)n-NR R (R and R are lower alkyl or bonded to form heterocylic ring; n is 1-4)] is reacted with a tertiary butyl compound/or isobutylene shown by the formula (CH3)3CX (X is halogen, O-functional group or N-functional group)] in the presence of Friedel-Craft catalyst (e.g. ferric chloride) at -50-150 deg.C to give a 5-tertiary butylsalicyclic acid derivative shown by formula III. Then this derivative is reacted with a propionyl halide shown by the formula C2H5COY (Y is halogen) in the same system to give the aimed substance shown by formula III.
-
公开(公告)号：JPS60237041A
公开(公告)日：1985-11-25
申请号：JP4108084
申请日：1984-03-02
摘要： PURPOSE:To obtain the titled compound industrially in high yield and purity by easy operation in short steps, by carrying out the Friedel-Crafts reaction using a specific salicylic acid derivative and a propionyl halide as starting materials, and diazo decomposition, etc. CONSTITUTION:A salicylic acid derivative of formula I {R is H or lower alkyl; R is -NH2 or -NHSO2R (R is aryl), -SO2R (R is the same as R ), -SR [R is R or -SR (R is the same as R )], -OSO2R (R is the same as R ) or formula II (R is the same as R )} and a propionyl halide are subjected to the Friedel-Crafts reaction or Fries rearrangement reaction to give a 3-propoinylsalicylic acid derivative of formula III (R ' is -NHCOC2H5, -NHSO2R , -SO2R , -SR , -OSO2R or formula II), which is then subjected to diazo decomposition or reduction to afford the aimed compound of formula IV. USE:A synthetic intermediate for flavoxate hydrochloride having pharmacological action, e.g. increasing the volume of urinary bladder and improving cysterethism, etc.
-
公开(公告)号：JPS5724362A
公开(公告)日：1982-02-08
申请号：JP9845980
申请日：1980-07-17
IPC分类号： C07D263/24 , C07D209/08 , C07D209/43 , C07D413/12
摘要： PURPOSE: To obtain the titled compound useful as a β-sympatholytic agent in high purity and in high yield, by reducing β-(4-indolyloxy)lactisopropylamide as a raw material by a short process and simple operations.
CONSTITUTION: β-(4-Indolyloxy)lactisopropylamide shown by the formula I as a raw material is reduced in the presence of a reducing catalyst, e.g., aluminum borohydride, sodium boron hydride, etc. in an inert solvent, e.g., tetrahydrofuran, etc. at 0W50°C, preferably at 10W30°C, to give a compound shown by the formula II. The compound shown by the formula I is a novel compound, which is obtained by reacting a compound shown by the formula III with a compound shown by the formula IV to give novel β-(4-indolyloxy)lactic acid shown by the formula V, which is easily reacted with isopropylamine.
COPYRIGHT: (C)1982,JPO&Japio摘要翻译： 目的：通过短程和简单的操作，通过还原β-（4-吲哚氧基）乳丙酯酰胺作为原料，得到高纯度，高收率的β-交替溶解剂有用的标题化合物。 构成：在惰性溶剂（例如四氢呋喃等）中，在还原催化剂例如硼氢化钠，硼氢化钠等的存在下还原作为原料的式I所示的β-（4-茚基氧基）乳状异丙基酰胺 在0-50℃，优选10-30℃，得到式II所示的化合物。 式I所示的化合物是通过使式III所示的化合物与式IV所示的化合物反应而得到的新化合物，得到式V所示的新的β-（4-二烯基氧）乳酸， 其容易与异丙胺反应。
-
-
-
-
-
-
-
-
-
搜索结果
12 条记录 (耗时 0.019 秒)
