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1. 发明专利

JPH01308270A PRODUCTION OF 1,2,4-THIAZIAZOLE-5-THIOL OR SALT THEREOF 失效
公开(公告)号：JPH01308270A
公开(公告)日：1989-12-12
申请号：JP13795688
申请日：1988-06-03
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MUKUDA TAKASHI , UEMATSU RYOICHI , HIRABAYASHI SATOSHI
IPC分类号： C07D285/08
摘要： PURPOSE:To obtain the title compound useful as a synthetic raw material for beta-lactam based antibiotic in one process, high yield and low cost, by reacting formamidine, or salt thereof with a xanthic acid O-ester and sulfur using the above-mentioned compounds as raw materials. CONSTITUTION:Formamidine or salt thereof is reacted with xanthic acid O-ester or salt thereof and sulfur normally in a solvent such as water, acetone or chloroform at ambient temperature or while heating to provide the aimed compound. The xanthic acid O-ester includes O-alkylxanthic acid such as O-methylxanthic acid, especially preferably 1-6C alkylxanthic acid. Further, the xanthic acid O-ester and salt thereof can be readily synthesized from carbon disulfide and alcoholic base and can be reacted with formamidine after isolating or without isolating.

2. 发明专利

JPH0318609B2 失效
公开(公告)号：JPH0318609B2
公开(公告)日：1991-03-13
申请号：JP16282282
申请日：1982-09-18
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： YAZAWA HISATOYO , MUKUDA TAKASHI , KONO KEIKO
IPC分类号： C07D501/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/02 , C07C233/07 , C07D257/04 , C07K1/10

3. 发明专利

JPH0625102B2 失效
公开(公告)号：JPH0625102B2
公开(公告)日：1994-04-06
申请号：JP12218791
申请日：1991-04-23
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： ZANKA ATSUHIKO , MUKUDA TAKASHI , HIRABAYASHI SATOSHI
IPC分类号： C07C303/38 , A61K31/18 , C07C20060101 , C07C43/257 , C07C303/40 , C07C311/08 , C07C311/09 , C07C319/06 , C07C319/18 , C07C323/09 , C07C323/37 , C07C323/49 , C07C323/63

4. 发明专利

JPH04312559A PRODUCTION OF 4-ALKANOYL-2-HALOANILINE 失效
公开(公告)号：JPH04312559A
公开(公告)日：1992-11-04
申请号：JP10664491
申请日：1991-04-10
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： ZANKA ATSUHIKO , HIRABAYASHI SATOSHI , MUKUDA TAKASHI , KUBOTA ARIKATSU
IPC分类号： C07C221/00 , C07C225/22
摘要： PURPOSE:To industrially and advantageously obtain 4-alkanoyl-2-haloanilines useful as an intermediate for alkanesulfonanilide derivatives having pharmacological actions such as anti-inflammatory and analgesic actions by using a stable halogenating reagent. CONSTITUTION:A 4-alkanoylaniline or its salt is reacted with an N- halosuccinimide stable to heat, shock, etc., in the presence of an aromatic amine according to a conventional method to selectively halogenate the 2-position of the 4-alkanoylaniline. Thereby, the objective 4-alkanoyl-2-haloaniline or its salt is industrially and advantageously obtained.

5. 发明专利

JP2000080072A PRODUCTION OF L-ARGININE 失效
公开(公告)号：JP2000080072A
公开(公告)日：2000-03-21
申请号：JP18860599
申请日：1999-07-02
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MUKAI KOJI , MUKUDA TAKASHI , KAWAKAMI RYOICHI
IPC分类号： C07C277/08 , C07C279/14
摘要： PROBLEM TO BE SOLVED: To obtain L-arginine having a small crystal particle size distribution width in good particle size distribution repeatability and suitable for powder filling treatments by adding a specific amount of L-arginine crystals as seed crystals to a supersaturated solution of the L-arginine, when the L-arginine is crystallized. SOLUTION: This method for producing arginine crystals comprises crystallizing L-arginine. Therein, L-arginine crystals are added as seed crystals to the supersaturated solution of the L-arginine. The L-arginine crystals use for the seed crystals are preferably particulate L-arginine which has an average particle diameter of 100-300 μm and to which many fine L-arginine crystals (preferably fine L-arginine crystals having a particle diameter of 0.5-2 μm in an amount of 1×109 to 1×1011 crystals/g of the seed crystals) are preferably adhered as secondary nuclei used as the crystallization of the L-arginine. The L-arginine crystals used as the seed crystals may be fine L-arginine crystals obtained by grinding L-arginine crystals by the use of a grinder, etc., and having a particle diameter of 0.5-2 μm.

6. 发明专利

JPH064640B2 失效
公开(公告)号：JPH064640B2
公开(公告)日：1994-01-19
申请号：JP13245684
申请日：1984-06-26
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： YAZAWA HISATOYO , ICHIHARA MASAHARU , KAGARA KOJI , MUKUDA TAKASHI
IPC分类号： C07D501/04

7. 发明专利

JPH051023A PRODUCTION OF ALKANESULFONANILIDE DERIVATIVE 失效
公开(公告)号：JPH051023A
公开(公告)日：1993-01-08
申请号：JP12218791
申请日：1991-04-23
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： ZANKA ATSUHIKO , MUKUDA TAKASHI , HIRABAYASHI SATOSHI
IPC分类号： C07C303/38 , A61K31/18 , C07C20060101 , C07C43/257 , C07C303/40 , C07C311/08 , C07C311/09 , C07C319/06 , C07C319/18 , C07C323/09 , C07C323/37 , C07C323/49 , C07C323/63
摘要： PURPOSE:To produce an alkanesulfoneanilide derivative or salt thereof having antiphlogistic action and analgesic action from a new raw material, in reduced producing processes and good yield. CONSTITUTION:A new compound expressed by formula I (R is lower alkyl; R is CN, CONH2 or lower alkanoyl; X is halogen) or salt thereof is reacted with a compound expressed by formula II (R and R are halogen; A is O or S; M is H, alkali metal or Cu) or salt thereof in the presence of a copper-base catalyst and a base using an aromatic amine based solvent to directly provide a compound expressed by formula III or salt thereof in high yield without using a preliminary process required in a conventional method. Furthermore, the new above-mentioned raw material can be produced by reacting a compound expressed by formula IV, its reactive derivative of the amino group or salt thereof with a compound expressed by the formula R SO2OH, its reactive derivative of the sulfonic acid group or salt thereof to give a compound expressed by formula V or salt thereof and then hologenating the compound expressed by formula V or salt thereof.

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