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1. 发明专利

JPS60104099A NOVEL PREPARATION OF COMPOUND RELATED TO SPERGUALIN 失效
公开(公告)号：JPS60104099A
公开(公告)日：1985-06-08
申请号：JP20909983
申请日：1983-11-09
申请人： NIPPON KAYAKU KK , TAKARA SHUZO CO
发明人： YOSHIDA MASAO , TOMIYOSHI TSUGIO , TAKEI MASAO , SAINO TETSUYUKI , NISHIZAWA RINZOU , NAKAMURA TERUYA , UMEZAWA HAMAO
IPC分类号： C07K1/00 , C07C67/00 , C07C239/00 , C07C277/08 , C07C279/14 , C07K1/113 , C07K5/02
摘要： PURPOSE:To obtain a 10-[-N(omega-guanidinoacyl)-aminoacyl]-1,5,10-triazadecane derivative useful as an antitumor agent in high yield, by guanidinating a specific novel intermediate, deprotecting a protecting group. CONSTITUTION:A novel 10-[N-(omega-aminoacyl)-aminoacyl]-1,5-diprotected 1,5,10- triazadecane shown by the formula I (R1' is residue obtained by removal of one H from amino group and of OH from COOH of glycine or serine, and R1', neighboring carbonyl group and amino group form acid amide bond; R2 is amino-protecting group; m is 6-8) is guanidinated with O-methylisourea, etc. preferably at 9-11pH at room temperature - the boiling temperature of a solvent for 5-48hr, the protecting groups are removed, to give the desired compound shown by the formula II (R1 is R1'). The novel compound shown by the formula I is prepared by condensing a compound shown by the formula III (R3 is protecting group with a compound shown by the formula IV (to give a novel compound shown by the formula V, removing the protecting group R3 of the compound shown by the formula V.

2. 发明专利

JPS6015425A PRODUCTION OF POLYLYSINE 失效
公开(公告)号：JPS6015425A
公开(公告)日：1985-01-26
申请号：JP12238883
申请日：1983-07-07
申请人： NIPPON KAYAKU KK
发明人： SUGIMURA HIDEO , NISHIZAWA RINZOU
IPC分类号： C08G69/10 , C08G69/00
摘要： PURPOSE:To obtain polylysine of a uniform MW and a desired average MW in good reproducibility by a simple operation, by polymerizing an N -carboxy anhydride of an N -protected lysine in a specified solvent mixture and removing the protective groups. CONSTITUTION:An N -carboxy anhydride of N -protected lysine is polymerized in a solvent mixture containing at least one member selected from the group consisting of esters, hydrocarbons, halohydrocarbons, dioxane, and methyl ethyl ketone and at least one member selected from the group consisting of N-substituted aliphatic amides, dimethyl sulfoxide, acetone, and tetrahydrofuran, and the protective groups are removed. The isolation of the poly-N -protected lysine obtained by the polymerization can be effected by, for example, adding dilute hydrochloric acid to the polymerization reaction solution and filtering off the separated precipitate. It is possible to obtain polylysine from the poly-N - protected lysine by, for example, removing the protective groups by a method commonly used in peptide chemistry.

3. 发明专利

JPS5695158A PREPARATION OF NNCARBAMOYLLPPHYDROXYPHENYLGLYCINE 失效
公开(公告)号：JPS5695158A
公开(公告)日：1981-08-01
申请号：JP15291979
申请日：1979-11-28
申请人： NIPPON KAYAKU KK
发明人： NISHIZAWA RINZOU , TAKEI MASAO , HAGITA KAZUTERU , YOSHIDA MASAO
IPC分类号： C07C275/24
摘要： PURPOSE:To obtain the titled compound useful as intermediate for producing beta- lactam antibiotics readily and directly in high yield and in high purity, by reacting p-hydroxymandelic acid or its salt with an inexpensive urea. CONSTITUTION:p-Hydroxymandelic acid, or its salt is reacted with urea in water, water-containing organic solvent, or organic solvent, in pH1.5-11, preferably in pH2-8, to give the titled compound. Water is preferable as the solvent from economical point of view, and in the use of water the reaction solution is optionally concentrated and adjusted with an acid to pH1-2. The adjusted solution is cooled to deposit precipitated, which are filtered to isolate the titled compound. EFFECT:D-Isomer of p-hydrophenylglycine is useful as a raw material for antibiotics, and the titled compound can be transferred directly to the process of optical resolution by using an optical active amine.

4. 发明专利

JPS55145650A INTERMEDIATE AND ITS PREPARATION 失效
公开(公告)号：JPS55145650A
公开(公告)日：1980-11-13
申请号：JP5261579
申请日：1979-04-28
申请人： NIPPON KAYAKU KK
发明人： SAINO TETSUYUKI , NISHIZAWA RINZOU , SEYA KENJI , KATOU KUNIMOTO , TAKITA TOMOHISA , UMEZAWA HAMAO
IPC分类号： C07D263/16 , C07C67/00 , C07C231/00 , C07C231/12 , C07C231/18 , C07C233/47 , C07C233/83 , C07C233/84 , C07C233/87 , C07C301/00 , C07C303/28 , C07C309/66
摘要： NEW MATERIAL:A (2R,3R)- or (2R,3S)-3-aminopropionic acid ester derivative of formula I (X is Cl, etc.; R1 is lower alkyl, etc.; R2 is lower alkyl, etc.; R3 is ester residue) and a (4R,5S)- or (4S,5S)-oxazoline derivative of formula II. EXAMPLE:(2R,3R)-N-Benzoyl-3-amino-2-chloro-4-phenylbutyric acid methyl ester. USE:Synthetic intermediate of bestacin having a promoting activity of immunofunction, or its related compounds. PROCESS:A compound of formula I is obtained by the treatment of a (2R,3R)- or (2R,3S)-3-amino-2-hydroxypropionic acid ester derivative of formula III with methanesulfonyl chloride in the presence of a thionyl chloride or an organic base.

5. 发明专利

JPS5527153A PRODUCTION OF 3*55DIMETHYLL44LOWER ALKOXYCARBONYL PHTHAILC ANHYDRIDE 失效
公开(公告)号：JPS5527153A
公开(公告)日：1980-02-27
申请号：JP10007078
申请日：1978-08-18
申请人： NIPPON KAYAKU KK
发明人： KOSHIGOE TAICHI , TAKEI MASAO , FUJII TADASHI , NISHIZAWA RINZOU
IPC分类号： C07D307/89
摘要： PURPOSE:An acid anhydride is made to react with a lower alkyl ester of isodehydroacetic acid to give title compound useful as an synthetic intermediate of phthalazone derivatives used as a drug for cerebral thrombosis and hemorrhage because of its activity of inhibiting blood platelet coagulation. CONSTITUTION:The reaction between an acid anhydride of formula I (A is a group of formula II or III; X is halogen) and a lower alkyl ester of isodehydroacetic acid of formula IV (R is lower alkyl of 1-6 carbon atoms) is effected at 50- 250 deg.C to give title compound of formula V with high safety in one stage process. The process is unnecessary for using toxic and decomposable substances that have been used in the conventional processes and consists of reduced steps. The acid anhydride is, e.g., a monohalide of maleic anhydride.

6. 发明专利

JPS58116471A 4-HYDROXYMETHYL-1-PHTHALAZONE ESTER DERIVATIVE AND ITS ESTER 失效
公开(公告)号：JPS58116471A
公开(公告)日：1983-07-11
申请号：JP21044881
申请日：1981-12-29
申请人： NIPPON KAYAKU KK , BANYU PHARMA CO LTD
发明人： ISHIKAWA MASAYUKI , ITOU SHIGERU , YOSHIZAWA JIYUNJI , TAKEZAWA HIROSHI , IHARA MASAKI , NISHIZAWA RINZOU , SUGIMURA HIDEO , YOSHIDA MASAO
IPC分类号： A61K31/50 , A61K31/502 , A61K31/675 , A61P7/02 , A61P9/12 , C07D237/32 , C07F9/6509
摘要： NEW MATERIAL:A 4-hydroxymethyl-1-phthalazone ester derivative shown by the formulaI[R1 is alkyl; R2 is -SO3H, a group shown by the formula II(R3 is H, alkyl, ester, etc.), -CO-W (W is cyclic imine), -CO-X(Z)-Y (X is the residue obtained by removing 3 H from alkane, etc., one of Y and Z is H, carboxyl, etc., and the other is carboxyl, -N(R4)R5] and its salt. EXAMPLE:4-Hydroxymethyl-6,8-dimethyl-7-ethoxycarbonyl-1-phthalazone sulfuric ester. USE:A remedy for cerebral apoplexy, cerebral thrombosis, pultaceous induration, etc., having extremely powerful inhibiting action on blood platelet aggregation, inhibiting action on phosphodiesterase, etc. Usable as orally absorbable drug or injection. PROCESS:For example, 4-hydroxymethyl-1-phthalazone derivative shown by the formula III is sulfated, to give a compound shown by the formulaI.

7. 发明专利

JPS5636465A PHTHALAZONEE44HYDROXYACETIC ACID DERIVATIVE* ITS PREPARATION AND PRODUCTION OF 44HYDROXYMETHYLPHTHALAZONE DERIVATIVE 失效
公开(公告)号：JPS5636465A
公开(公告)日：1981-04-09
申请号：JP9676479
申请日：1979-07-31
申请人： NIPPON KAYAKU KK
发明人： TAKEI MASAO , YOSHIDA MASAO , NISHIZAWA RINZOU
IPC分类号： C07D237/32 , A61K31/50 , A61K31/502 , A61P7/02 , A61P25/28 , A61P43/00
摘要： NEW MATERIAL:6, 8-Dimethyl-7-alkyloxycarbonyl-1-phthalazone-4-alpha-hydroxyacetic acid of formula I (R is lower alkyl). EXAMPLE:6, 8-Dimethyl-7-ethoxycarbonyl-1-phthalazone-4-alpha-hydroxyacetic acid. USE:They are used as a synthetic intermediate of 4-hydroxymethylphthalazone derivatives that are used as a remedy for cerebral hemorrhage, cerebral thrombosis and pultaceous sclerosis, because of their high activity of inhibiting blood platelet coagulation and of inhibiting phosphodiesterase. These effectiveness can be expected too. PREPARATION:6, 8-Dimethyl-7-alkyloxycarbonyl-1-phthalazone-4-alpha-halogenoacetic acid of formula II is hydrolyzed in a neutral or basic medium to give the compound of formula I. 4-Hydroxymethylphthalazone derivatives are obtained by decarboxylation of the compound of formula I.

8. 发明专利

JPS5455712A DOUBLE SALT OF HALOGENATED METHYLMETHIONINE SULFONIUM AND ZINC HALIDE* AND ITS PREPARATION 失效
公开(公告)号：JPS5455712A
公开(公告)日：1979-05-04
申请号：JP12151877
申请日：1977-10-12
申请人： NIPPON KAYAKU KK
发明人： NISHIZAWA RINZOU , SUZUKI MASAO
IPC分类号： C07C381/12 , C07C67/00 , C07C325/00
摘要： NEW MATERIAL:Double salt of halogenated methylmethionine sulfonium of formula (x, y are Cl, Br) and zinc halide. USE:Non-hygroscopic vitamin U (remedy for acute or chronic gastritis, peptic or doudenal ulcer, hyperacidity, etc.). PROCESS:The compound can be prepared either (1) by reacting halogenated methylmethionine sulfonium with zinc halide in water or in a water-containing hydrophilic solvent pref. at 0-40 deg.C, followed by filtering the precipitated crystals, or (2) by mixing a solution containing methylmethionine sulfonium ion with a Zn salt such as zinc sulfate and a halogen ion-containing salt such as alkali halide, followed by filtering the precipitated crystals.

9. 发明专利

JPS5424847A OPTICAL ACTIVE METHIONINEEMANDELIC ACID COMPLEX AND ITS PREPARATION 失效
公开(公告)号：JPS5424847A
公开(公告)日：1979-02-24
申请号：JP8931177
申请日：1977-07-27
申请人： NIPPON KAYAKU KK
发明人： TASHIRO YASUHISA , NAGASHIMA KOUJI , AOKI SHIGERU , NISHIZAWA RINZOU
IPC分类号： C07C323/58 , C07C67/00 , C07C313/00
摘要： PURPOSE:Optical active methionine-mandelic acid complex of formula.

10. 发明专利

JPS60104053A NOVEL PROCESS FOR PRODUCING SPERMIDINE DERIVATIVE 失效
公开(公告)号：JPS60104053A
公开(公告)日：1985-06-08
申请号：JP20909883
申请日：1983-11-09
申请人： NIPPON KAYAKU KK , TAKARA SHUZO CO
发明人： TOMIYOSHI TSUGIO , YOSHIDA MASAO , SAINO TETSUYUKI , TAKEI MASAO , NISHIZAWA RINZOU , NAKAMURA TERUYA , UMEZAWA HAMAO
IPC分类号： C07C231/00 , C07C67/00 , C07C231/12 , C07C235/10
摘要： PURPOSE:To produce the titled compound useful as an intermediate of spergualin, by removing the acyl group of novel 10-[N-(alpha,alpha-diacyloxy)-1,5-diprotected-1, 5-diprotected-1,5,10-triazadecane] by hydrolysis, and eliminating the amino-protecting group. CONSTITUTION:The objective compound of formula II is produced by removing the acyl group of the novel compound of formula I (Ac is acyl; P1 and P2 are amino-protecting group) by hydrolysis, and if P1 and P2 are amino-protecting group, removing the P1, etc. The acyl group of the compound of formula I can be removed easily under mild condition without causing the decomposition of the amide bond. The hydrolysis is carried out preferably in a water-miscible solvent (e.g. methanol) using an aqueous solution of an inorganic base or a mineral acid at 10-40 deg.C. The condensation reaction of the compound of formula II with 3- hydroxy-7-guanidinoheptanoic amide gives spergualin useful as an antibacterial agent, etc.

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