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1. 发明专利

JPS6011450A PRODUCTION OF DIAZOMETHANE DERIVATIVE 失效
公开(公告)号：JPS6011450A
公开(公告)日：1985-01-21
申请号：JP11989483
申请日：1983-06-30
申请人： TAOKA CHEMICAL CO LTD
发明人： KOUNO KORETOMO , HIRAYAMA YOSHIHIKO , SAKAI TAMIO , SHIRAISHI YOSHIHISA , SAIJIYOU SHIGEYA
IPC分类号： C07C245/14 , C07C67/00 , C07C241/00 , C07C245/16 , C07C113/02
摘要： PURPOSE:To obtain the titled compound useful as a carboxyl-protecting group of organic compounds, in high yield and purity, by subjecting the solution containing a diazomethane derivative and an organic solvent to the continuous thin-layer evaporation concentration process under specific pressure and temperature condition. CONSTITUTION:A solution containing the diazomethane derivative of formula (R1 and R2 are substituted or unsubstituted aromatic group) and an orgnaic solvent (e.g. methylene chloride) is subjected to the continuous thin-layer evaporation concentration process under a vacuum of >=37cmHgG at

2. 发明专利

JPS6011449A STORAGE OF DIAZOMETHANE DERIVATIVE 失效
公开(公告)号：JPS6011449A
公开(公告)日：1985-01-21
申请号：JP11989383
申请日：1983-06-30
申请人： TAOKA CHEMICAL CO LTD
发明人： KOUNO KORETOMO , HIRAYAMA YOSHIHIKO , SAKAI TAMIO , SHIRAISHI YOSHIHISA , SAIJIYOU SHIGEYA
IPC分类号： C07C245/14 , C07C67/00 , C07C241/00 , C07C113/02
摘要： PURPOSE:To store the titled compound useful as a carboxyl-protecting group of organic compounds, easily, at a low cost, in high stability, by mixing a diazomethane derivative with methylene chloride at a specific ratio, and storing the mixture at a specific temperature. CONSTITUTION:The diazomethane derivative of formula (R1 and R2 are substituted or unsubstituted aromatic group) is mixed with methylene chloride at a weight ratio of (100-25):(0-75), and stored at -25-+15 deg.C, preferably, -20- +10 deg.C. Although diazomethane derivative is useful as a protecting group of the carboxyl of organic compounds, it is decomposed extremely easily, for example, diphenyldiazomethane is decomposed to ketazine when left at room temperature for 2 days, and the purity decreases to 75% of the original purity. It has been found that the decomposition rate of the compound can be decreased remarkably when the diazomethane derivative is stored in a state containing at least part of the diazomethane derivative in the form of crystal and in the presence of methylene chloride.

3. 发明授权

US4266000A Photosensitive copying composition 失效
标题翻译：感光复印组合
公开(公告)号：US4266000A
公开(公告)日：1981-05-05
申请号：US943193
申请日：1978-09-18
申请人： Paul Stahlhofen , Fritz Erdmann
发明人： Paul Stahlhofen , Fritz Erdmann
IPC分类号： C08K5/00 , C08K5/22 , C08L61/00 , C08L61/04 , C09B53/00 , G03C1/72 , G03F7/022 , H01L21/027 , H05K3/00 , C07C113/02 , G03C1/52
CPC分类号： G03F7/022
摘要： This invention relates to a photosensitive copying composition comprising a solvent and a naphthoquinone-(1,2)-diazidesulfonic acid ester as the photosensitive compound, said naphthoquinone diazide sulfonic acid ester having the general formula I ##STR1## wherein: X is a single bond or one of the groups ##STR2## R.sup.1, R.sup.1' and R.sup.1" are the same or different and are H or D, R.sup.2 and R.sup.2' are the same or different and are H or halogen,R.sup.3 is halogen or D, andD is a naphthoquinone-(1,2)-diazidesulfonyloxy group.
摘要翻译：本发明涉及一种含有溶剂和萘醌 - （1,2） - 二叠氮磺酸酯作为光敏化合物的感光复印组合物，所述萘醌二叠氮磺酸酯具有通式Ⅰ其中：X为单键或CO，CH 2，S，SO 2或R 1'之一可以相同或不同，为H或D，R2和R2'相同或不同，为H或卤素，R3为卤素或D，D为萘醌 - （1,2） - 二叠氮基磺酰氧基。

4. 发明授权

US3872076A 16-Diazoketones of the androstane, pregnane, estrane, and 19-norpregnane series 失效
标题翻译：雄甾烷，孕烷，雌激素和19-去甲孕烷系列的16-重氮酮
公开(公告)号：US3872076A
公开(公告)日：1975-03-18
申请号：US21795672
申请日：1972-01-14
申请人： HOFFMANN LA ROCHE
发明人： ROSEN PERRY
IPC分类号： C07C62/00 , C07D307/77 , C07J73/00 , C07C113/02 , A61K17/06
CPC分类号： C07D307/77 , C07C62/00 , C07C2603/26 , C07J73/003 , Y10S514/874
摘要： 15-Oxasteroids of the androstane, pregnane, estrane, and 19norpregnane series are useful as hormonal agents.
摘要翻译：雄甾烷，孕烷，雌激素和19-去甲孕烷系列的甾体化合物可用作激素剂。

5. 发明专利

DK139067B 未知
公开(公告)号：DK139067B
公开(公告)日：1978-12-11
申请号：DK379673
申请日：1973-07-09
申请人： GLAXO LAB LTD
发明人： GALLAGHER GERARD , WALKER DEREK , EASTLICK DAVID THOMAS
IPC分类号： C07C20060101 , C07D307/52 , C07D333/22 , C07C113/02

6. 发明专利

GB1459606A PHTHALAZONE COMPOUNDS 未知
公开(公告)号：GB1459606A
公开(公告)日：1976-12-22
申请号：GB3870874
申请日：1974-09-04
申请人： INOUE M ISHIKAWA M TSUCHIYA T , SHIMAMOTO TAKIO
IPC分类号： C07D307/89 , C07D491/048 , C07D237/32 , A61K31/495 , C07D491/04 , C07C69/76 , C07C113/02 , C07D309/10 , C07D307/88
摘要： 1459606 4-Hydroxymethylphthalazones M INOUE M ISHIKAWA T TSUCHIYA and T SHIMAMOTO 4 Sept 1974 [30 Oct 1973 31 Oct 1973] 38708/74 Heading C2C The invention comprises compounds of Formula I in which R 1 and R 2 are independently C 1-3 alkyl and R 3 is C 1-5 alkyl or R 2 and R 3 together form a methylene, ethylidene or propylidene group which may be prepared by (a) reacting a compound of Formula II wherein R 1 , R 2 and R 3 are as defined above and Z is alkoxy, halogen, O.CO.O.CH 3 or with an alkali metal borohydride in the presence or absence of a metal halide or (b) reacting a compound of Formula III with hydrazine. The methyl and ethyl esters of 6-carboxy-5,7- dimethyl - 3 - hydroxy - 3 - methylphthalide are prepared by heating the methyl and ethyl esters of 5-carboxy-4,6-dimethylbenzene-1,2-dicarboxylic acid anhydride with malonic acid and pyridine and are reacted with hydrazine to obtain 6,8 - dimethyl - 7 - methoxycarbonyl (or ethoxycarbonyl) - 1 - phthalazone - 4 - carboxylic acid which are in turn esterified by heating with ethanol and concentrated sulphuric acid to obtain the corresponding diesters. 3,5 - Dimethyl - 4,6 - diethoxycarbonylbenzoic acid is refluxed with thionyl chloride to obtain 3,5 - dimethyl - 4,6 - diethoxycarbonylbenzoylchloride which is further reacted with diazomethane to obtain 3,5-dimethyl-4,6-diethoxycarbonyl-w-diazoacetophenone which is cyclized by heating with sulphuric acid in dioxane to obtain 6,8 - dimethyl - 7 - ethoxycarbonyl isochroman-1,4-dione. 8 - Bromomethyl - 4,7 - diethoxycarbonyl - 6- methyl - 1 - phthalazone, obtained by reaction of 6,8 - dimethyl - 4,7 - diethoxycarbonyl - 1 - phthalazone with N-bromosuccinimide and benzoyl peroxide, is heated under vacuum to obtain a compound of the Formula IV 6,8 - Dimethyl - 7 - ethoxycarbonyl - 4 - hydroxymethyl - 1 - phthalazone is refluxed with trifluoroacetic acid to obtain 6,8-dimethyl-7- carboxy - 4 - hydroxymethyl - 1 - phthalazone. Pharmaceutical compositions having activity in the treatment of hypertensive, atherosclerotic and thrombotic diseases and diseases due to misfunction of the cyclic AMP for oral or parenteral administration comprise a phthalazone derivative of Formula I and a pharmaceutically acceptable diluent or carrier.

7. 发明专利

GB1442755A DIAZO COMPOUNDS 未知
公开(公告)号：GB1442755A
公开(公告)日：1976-07-14
申请号：GB3242372
申请日：1972-07-11
申请人： GLAXO LAB LTD
IPC分类号： C07D333/22 , B01J21/00 , B01J31/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C241/00 , C07C245/12 , C07C245/14 , C07C313/00 , C07C317/28 , C07C317/30 , C07D207/335 , C07D213/53 , C07D307/52 , C07C113/02
摘要： 1442755 Diazo compounds GLAXO LABORATORIES Ltd 10 July 1973 [11 July 1972] 32423/72 Heading C2C The invention comprises a process for the preparation of a diazo compound of the formula (where R 1 is a hydrogen atom or R, where R is an aryl, aralkyl, 5- or 6-membered heterocyclic, heterocyclic-substituted alkyl, alkyl or cycloalkyl group, which groups are unsubstituted or substituted by one or more halogen atoms or cyano, nitro, alkyl, alkylsulphonyl or alkoxy groups; R 2 has independently any of the defined meanings for R; or where R 1 and R 2 together with the intervening carbon atom form a cyclic hydrocarbon group which may be interrupted by one of more of O or N) which comprises reacting a hydrazone of the formula (where R 1 and R 2 are as defined above) with an oxidizing agent in the presence of a base, said oxidizing agent comprising an organic peracid, periodic acid, a hypohalous acid, a hypohalite salt or ester, chlorine, bromine or chromic acid. In a modification the hydrazone starting material may be substituted by a further hydrazone-carrying group. The diazo compounds may be used to esterify penicillin compounds.

8. 发明专利

ATA602173A 未知
公开(公告)号：ATA602173A
公开(公告)日：1976-04-15
申请号：AT602173
申请日：1973-07-09
申请人： GLAXO LAB LTD
IPC分类号： C07D333/22 , B01J21/00 , B01J31/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C241/00 , C07C245/12 , C07C245/14 , C07C313/00 , C07C317/28 , C07C317/30 , C07D207/335 , C07D213/53 , C07D307/52 , C07C113/02

9. 发明专利

GB1369800A ANTI-HYPERGLYCEMIC PREPARATIONS AND METHODS OF TREATMENT 未知
公开(公告)号：GB1369800A
公开(公告)日：1974-10-09
申请号：GB5833271
申请日：1971-12-15
申请人： UPJOHN CO
IPC分类号： C07C69/753 , A61K27/00 , C07C47/38 , C07C61/00 , C07C69/74 , C07C113/02
摘要： 1369800 Carboxy-bicyclo-alkenes and -alkanes and derivatives thereof UPJOHN CO 15 Dec 1971 [14 Jan 1971] 58332/71 Heading C2C [Also in Division A5] The following reaction sequences are described: (A) Bicyclo[2.2.1] heptadiene is oxidized to bicyclo[3.1.0] hex-2-ene-6-endo-carbonaldehyde, which is oxidized to bicyclo[3.1.0] hex- 2-ene-6-endo-carboxylic acid, which is hydrogenated to bicyclo[3.1.0] hexane-6-endo-carboxylic acid which is etherified to methyl bicyclo- [3.1.0] hexane-6-endo-carboxylate which is deesterified to exo-bicyclo[3.1.0] hexane-6-carboxylic acid which is esterified using diazomethane to methyl exo-bicyclo[3.1.0] hexane-6- carboxylate. (B) Exo-bicyclo[3.1.0] hexane-6- formyl chloride is converted by diazomethane and a Wolf rearrangement to methyl exobicyclo[3.1.0] hexane-6-acetate which is deesterified to exo-bicyclo[3.1.0] hexane-6-acetic acid. (C) Exo-bicyclo[3.1.0] hexane-6-formyl chloride is esterified to ethyl exo-bicyclo[3.1.0]- hexane-6-carboxylate.

10. 发明专利

NL183457C 未知
公开(公告)号：NL183457C
公开(公告)日：1988-11-01
申请号：NL7309547
申请日：1973-07-09
申请人： GLAXO LAB LTD
IPC分类号： C07D333/22 , B01J21/00 , B01J31/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C241/00 , C07C245/12 , C07C245/14 , C07C313/00 , C07C317/28 , C07C317/30 , C07D207/335 , C07D213/53 , C07D307/52 , C07C113/02 , C07D333/20

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