公开(公告)号：JPS5579356A

公开(公告)日：1980-06-14

申请号：JP15319578

申请日：1978-12-13

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  SUGIHARA HIROSHI ,  MAZAKI MITSUO

IPC: C07C255/19 ,  C07C67/00 ,  C07C253/00

Abstract: PURPOSE:To obtain the title compounds useful as a raw material and intermediate, etc., for varieties of organic synthetic chemicals, e.g. medicines, agricultural chemicals, by reacting oxamidic acid esters, with phosgene or trichloromethyl chloroformate and a tertiary amine. CONSTITUTION:The compound of formula I (R is alkyl, cycloalkyl, or aralkyl, e.g. methyl oxamate, is reacted with phosgene of formula II or the compound of formula III, and a tertiary amine of formula IV, e.g. trimethylamine, in a solvent, e.g. benzene, at -20-150 deg.C, to obtain the compound of formula V, e.g. methyl cyanoformate. The compound thus formed is mixed with water, in the absence of solvents, and separated into the aqueous and non-aqueous layers, and the compound of the formula is isolated by distillation or recrystallization.

公开(公告)号：JPS53132586A

公开(公告)日：1978-11-18

申请号：JP4744877

申请日：1977-04-26

Applicant: UBE INDUSTRIES

Inventor： MAZAKI MITSUO ,  FUKUI KIYOSHI ,  KITA JIYUNICHIROU

IPC: C07D201/02

Abstract: PURPOSE:To prepare ?-caprolactam without ammonium sulfate by-production, from nitrobenzene, n-butanol, and tertiary lower-alkyl phosphine.

公开(公告)号：JPS5253878A

公开(公告)日：1977-04-30

申请号：JP12931875

申请日：1975-10-29

Applicant: UBE INDUSTRIES

Inventor： MAZAKI MITSUO ,  FUKUI KIYOSHI ,  KITA JIYUNICHIROU

IPC: C07D223/10

Abstract: PURPOSE:To prepare2-alkoxy-3H-azepines, which are useful as intermediates for blood sugar depressants, diuretics, antibacterial agents, etc., form easily available materials in high yields.

公开(公告)号：JPS63198983A

公开(公告)日：1988-08-17

申请号：JP3192887

申请日：1987-02-14

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  KUBO FUMIO ,  WATANABE MASAYUKI

IPC: C12N9/02

Abstract: PURPOSE:To produce recombinant human superoxide dismutase (SOD) containing theoretical amount of copper ion and having high enzyme activity, by treating a solution of apoenzyme containing no copper of recombinant human SOD or insufficient for the copper with a copper salt in the presence of beta- mercaptoethanol. CONSTITUTION:A microorganism transformed with recombinant DNA having a human superoxide dismutase (SOD) structural gene downstream plasma expressing regulatory gene is cultivated and induction synthesis of SOD is carried out to provide a humid germ cell, which is suspended in a proper water solution having 5-8pH, ground to afford supernatant. beta-Mercaptoethanol having 5-100mM concentration is added to the supernatant or supernatant, etc., obtained after treating precipitation of ammonium sulfate, and further a copper salt having anion of an organic or inorganic acid is added in a concentration of 0.15X10 -15X10 mol. based on 1g of the humid germ cell at 0 deg.C - room temperature and the mixture is allowed to stand or stirred at 0 deg.C - room temperature, preferably at low temperature of nearly 4 deg.C for 10min - 1 day to isolate the aimed SOD.

公开(公告)号：JPS5888381A

公开(公告)日：1983-05-26

申请号：JP18688881

申请日：1981-11-24

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  KAKEYA NOBORU ,  JIBIKI HIROSHI ,  MATSUO FUMIO

IPC: C07D487/04 ,  A01N43/90

Abstract: NEW MATERIAL:The compound of formulaI[R is H, 1-4C alkyl, phenyl, 2- 5C alkoxycarbonyl, benzoyl, etc.; R and R are H, 1-10C alkyl, allyl, cyclohexyl, benzyl, or group of formula V (R is 1-4C alkyl, 1-4C alkoxy, etc.; n is 0, 1 or 2)]. EXAMPLE:2-Cyclohexyl-1,2,3,5,6,7-hexahydro-1,3,5,7-tetraoxoimidazo-[1, 5-C]pyrimidine. USE:Pharmaceuticals, agricultural chemicals, and their intermediates. PROCESS:The objective compound of e.g. formula IV can be prepared by reacting the orotic acid ester of formula II (R is 1-4C alkyl) with the isocyanate of formula III (R is 1-10C alkyl, allyl, etc.) in the presence of a tertiary amine, etc.

公开(公告)号：JPS5862174A

公开(公告)日：1983-04-13

申请号：JP15949681

申请日：1981-10-08

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  KITA JIYUNICHIROU ,  FUJIMURA SUSUMU ,  OKIMOTO KIYOMI ,  JIBIKI HIROSHI

IPC: C07D487/04 ,  A01N43/90

Abstract: NEW MATERIAL:A pyrrolopyrimidine derivative shown by the formulaI(R and R are 1-4C alkyl, 2-4C alkenyl, 5-7C cycloalkyl, 7-10C aralkyl, or a group shown by the formula II; R is 1-4C alkyl, or halogen; n is 0-3). EXAMPLE:3,6-Dimethyl-2-hydroxy-3,4,6,7-tetrahydro-4,5,7-trioxo-5H-pyrr olo[3,4- d]pyrimidine. USE:Useful as an agricultural chemical, drug, or intermediate for them. PROCESS:For example, an aminomaleimide shown by the formula III is reacted with phosgene or chloroformic trichloromethyl ester in the presence of pyridine in a solvent such as benzene, etc. usually at -20-100 deg.C, to give a compound shown by the formulaI. In another method, a compound shown by the formula IV is subjected to ring closure in the presence of boron trifluoride under heating at 50-150 deg.C, to give the compound shown by the formulaI.

公开(公告)号：JPS5862166A

公开(公告)日：1983-04-13

申请号：JP15949481

申请日：1981-10-08

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  KITA JIYUNICHIROU ,  YOKOO YASUHIKO

IPC: C07D239/557 ,  A61K31/505 ,  C07D239/54

Abstract: NEW MATERIAL:A compound shown by the formulaI(R is 1-4C alkyl, or phenyl; R is 1-4C alkyl). USE:A drug, agricultural chemical and an intermediate for them. PROCESS:A compound shown by the formula II is reacted with phosgene or chloroformic trichloromethyl ester in a solvent, preferably sufficiently anhydrous aromatic hydrocarbon, halogenated hydrocarbon, etc. in the presence of pyridine at -20-40 deg.C for 1-30hr, to give a compound shown by the formulaI. The amount of pyridine used is preferably 2mol based on 1mol phsogene and 4mol based on 1mol chloroformic trichloromethyl ester. The amount of the compound shown by the formula II used is preferably 0.4-1mol based on 1mol phosgene and 0.2-0.5mol based on 1mol chloroformic trichloromethyl ester.

公开(公告)号：JPS5862165A

公开(公告)日：1983-04-13

申请号：JP15949881

申请日：1981-10-08

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  OKIMOTO KIYOMI

IPC: C07D233/96

Abstract: PURPOSE:To obtain the titled substance useful as a drug, agricultural chemical, their intermediates, etc. in high yield, by reacting amidinecarboxylic acid amide with phosgene or chloroformic trichloromethyl ester in the presence of pyridine. CONSTITUTION:A compound shown by the formulaI[R is 1-4C alkyl, 2-5C alkenyl, 5-7C cycloalkyl, or 7-10C aralkyl; R is R or a group shown by the formula II (R is 1-4C alkyl, or halogen; n is 0, 1, 2, or 3)]is reacted with phosgene or chloroformic trichloromethyl ester in the presence of pyridine at -20-40 deg.C for 1-24hr to give a compound shown by the formula III. In the reaction, a solvent such as an aromatic hydrocarbon, halogenated hydrocarbon, etc. which is sufficiently anhydrous is preperably used. The amount of pyridine used is 2mol based on 1mol phosgene and 4mol based on 1mol chloroformic trichloromethyl ester.

公开(公告)号：JPS5862149A

公开(公告)日：1983-04-13

申请号：JP15949381

申请日：1981-10-08

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  JIBIKI HIROSHI ,  OKIMOTO KIYOMI

IPC: A61K31/155 ,  A01N37/52 ,  A61K31/16 ,  A61K31/165 ,  C07C67/00 ,  C07C239/00 ,  C07C257/20

Abstract: NEW MATERIAL:The compound of formulaI[R is 1-20C alkyl, 2-5C alkenyl, 5-7C cycloalkyl, or 7-10C aralkyl; R is 1-4C alkyl, 1-4C halogenated alkyl, or group of formula II (X is halogen; n is 0, 1, 2 or 3)]. EXAMPLE:N-(n-Butyl)-N'-(2,4-dichlorobenzoyl)amidinecarboxylic acid (n-butyl)amide. USE:Useful as pesticides, pharmaceuticals, and their intermediates. PROCESS:The compound of formulaIis prepared by reacting the amidine-carboxylic acid amide of formula III with the carboxylic acid chloride of formula R -CO-Cl in the presence of a tertiary amine (e.g. trimethylamine) under essentially anhydrous condition at -20-+100 deg.C.

公开(公告)号：JPS5859967A

公开(公告)日：1983-04-09

申请号：JP15807681

申请日：1981-10-06

Applicant: UBE INDUSTRIES

Inventor： FUKUI KIYOSHI ,  KITA JIYUNICHIROU ,  FUJIMURA SUSUMU ,  MATSUO FUMIO

IPC: C07D207/456 ,  A01N37/32

Abstract: NEW MATERIAL:An aminomaleimide of formulaI[R is H, 1-4C alkyl, 2- 4C alkenyl, 5-7C cycloalkyl, 7-10C aralkyl, formula III (R is 1-4C alkyl, 1-4C alkoxy, halogen; n is 0, 1, 2, 3)]. EXAMPLE:3-Amino-4-carbamoylmaleimide. USE:Medicines, agricultural chemicals or their intermediate. PREPARATION:The reaction between a cyanoformic acid ester of N C-COOR R is 1-4C alkyl) and a bromomalonamide of formula II in the presence of stannous chloride is followed by treatment of the reaction product with water or an acidic aqueous solution to give the compound of formulaI.