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21. 发明专利

JPS5373593A PENICILLIN DERIVATIVES 失效
公开(公告)号：JPS5373593A
公开(公告)日：1978-06-30
申请号：JP15006176
申请日：1976-12-14
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , ITOU JINDOU , SHIRASAKA TADASHI
IPC分类号： C07D499/70 , A61K31/50 , A61P31/04 , C07D499/64
摘要： PURPOSE:Penicillin derivatives I and their salts (R1 is H or lower alkoxy; R2 is H or lower alkoxycarbonyl; X is H, OH or amino). E.f., 6-[D-2-(4-ethoxycarbonyloxyphthalazine-1-carboxyamide] penicillanic acid.

22. 发明专利

JPS5373592A PENICILLIN DERIVATIVES 失效
公开(公告)号：JPS5373592A
公开(公告)日：1978-06-30
申请号：JP15006076
申请日：1976-12-14
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , KOMATA KENZOU , ITOU JINDOU
IPC分类号： C07D499/70 , A61K31/505 , A61P31/04 , C07D499/64 , C07D499/68
摘要： PURPOSE:Penicillin derivatives I and their salts (R is H, lower alkyl, lower alkoxy or halogen; X is H, OH or amino). E.g., potassium 6-[D-2-[2-(3, 4dihydro -4-oxo-3-quinazolinyl)acetamide]-2-phenylacetamide] penicillanate' dihydrates.

23. 发明专利

JPS5373587A NEW PENICILLINE DERIVATIVES 失效
公开(公告)号：JPS5373587A
公开(公告)日：1978-06-30
申请号：JP14819176
申请日：1976-12-09
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , KOMATA KENZOU , OOYA JIYUNICHI
IPC分类号： C07D499/68 , A61K31/505 , A61P31/04 , C07D499/64
摘要： PURPOSE:Penicillin derivatives I and their salts (X is H or amino - protecting groups; Y is H, OH or amino). E.g., potassium 6-[D-2-(3-benzyloxycarbonyl6-oxo-4-hexahydropyrimidinylcarboxamide)-2- phenylacetamide] penicillanate'dihydrates.

24. 发明专利

JPS5340794A NOVEL PENICILLIN DERIVATIVES 失效
公开(公告)号：JPS5340794A
公开(公告)日：1978-04-13
申请号：JP11565076
申请日：1976-09-27
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , KOMATA KENZOU , OOYA JIYUNICHI , AZUMA KAZUO , SHIRASAKA TADASHI
IPC分类号： C07D499/68 , A61K31/43 , A61P31/04 , C07D499/64 , C07D499/70
摘要： PURPOSE:Penicillin derivatives of formula I(R is H, C1-5 lower alkyl, amino protecting group; R2 is H, C1-5 lower alkyl; R4, R5, and R6 are H, OH, C1-5 lower alkoxy, amino, halogen; R7 is H, alkali matal; with the proviso that R3 is lower alkyl when R1 and R2 are H), e.g. potassium 6-[D-2-(N-tosyl-Nmethyl-D-alanyl) amino-2-phenylacetamido] penicillanate monohydrate.

25. 发明专利

JPS5295688A NOVEL PENICILLIN DERIVATIVES 失效
公开(公告)号：JPS5295688A
公开(公告)日：1977-08-11
申请号：JP1212176
申请日：1976-02-06
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , KOMATA KENZOU , OOYA JIYUNICHI , AZUMA KAZUO , SHIROSAKA TADASHI
IPC分类号： C07D499/68 , A61K31/43 , A61P31/04 , C07D499/64
摘要： PURPOSE:Penicillin derivatives I (X is H or alkali metal), e.g. 6-[D-2(D-piperidine-2-carboxamido)-2-phenylacetamido]-penicillanic acid'tetrahydrate.

26. 发明专利

JPS5283570A THIOACETALS OF GLUTARIMIDOOBBACETALDEHYDES 失效
公开(公告)号：JPS5283570A
公开(公告)日：1977-07-12
申请号：JP21276
申请日：1976-01-01
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , AZUMA KAZUO
IPC分类号： C07D211/88
摘要： PURPOSE:Thioacetals of glutarimido-beta-acetaldehydes of formula I (R is H, acyl, alkyl, or aryl of less than 11 carbon atoms; R is alkyl or aryl of less than 11 carbon atoms); for example, dipheylthioacetal of glutalimido-beta-acetaldehyde of formula II.

27. 发明专利

JPH0511114B2 失效
公开(公告)号：JPH0511114B2
公开(公告)日：1993-02-12
申请号：JP18696385
申请日：1985-08-26
申请人： MITSUBISHI CHEM IND AMERIKA INC
发明人： MORITA YOSHIMI , IMAKI SUNAO , TAKAYANAGI HISAO , SHIRASAKA TADASHI
IPC分类号： C07D317/54 , C07D317/58 , C07D317/64

28. 发明专利

JPS62240663A HETEROCYCLIC THIOALANINE DERIVATIVE 失效
公开(公告)号：JPS62240663A
公开(公告)日：1987-10-21
申请号：JP8387786
申请日：1986-04-11
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , HOSHIIDE YASUO , TANIGUCHI SEIRO , OKADA KAZUO , ANDO RYOICHI , TAKASHIMA JUNKO
IPC分类号： C07K14/00 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/433 , A61P31/04 , C07D213/70 , C07D233/64 , C07D239/38 , C07D249/12 , C07D263/58 , C07D271/00 , C07D277/20 , C07D277/36 , C07D277/74 , C07D285/12 , C07D285/125 , C07K5/06
摘要： NEW MATERIAL:A compound of formula I (P is formula VI-VIII; Q is O, S, NR ; Z is N, CR ; R -R are H, alkyl, further R is H, alkyl; R and R incorporate to form alicyclic or aromatic ring; dotted line represents a bond existing in some cases; A is H, amino acid or oligopeptide which may have protecting group of the residue after removing OH from terminal CO2H or protecting group, B is OH, amino acid or oligopeptide residue which may have protecting groups after removing H from terminal NH2, protecting group). EXAMPLE:S-(2-Methyl-1,3,4-thiadiazol-5-yl)-D-cysteine. USE:A synthetic intermediate of inhibitor of cell wall biosynthesis and antibacterial agent. PREPARATION:The reaction of a compound of formula II (it is protected, when P contains functional groups active in the substitution reaction) with another compound of formula III (R is OH, protecting group) in the presence of a base is followed by deprotection, when necessary, to give a compound of formula V.

29. 发明专利

JPS62221676A 2-AMINOXYPROPIONIC ACID DERIVATIVE 失效
公开(公告)号：JPS62221676A
公开(公告)日：1987-09-29
申请号：JP6275786
申请日：1986-03-20
申请人： MITSUBISHI CHEM IND
发明人： MORITA YOSHIMI , TANIGUCHI SEIRO , CHAGI HARUYUKI
IPC分类号： C07D257/04 , A61K31/41 , A61P31/04 , C07K14/00
摘要： NEW MATERIAL:A 2-aminoxypropionic acid derivative of formula I (R is alkyl or aryl; Y is OH or carboxyl-protecting group; X is H or amono acid or oligopeptide residue obtained by removing OH of terminal carboxyl group from amino acid or oligopeptide). EXAMPLE:2-Aminoxy-3-(1-methyltetrazol-5-yl)thiopropionic acid. USE:An agent for inhibiting biosynthesis of bacterial cell wall and an antibacterial agent. PREPARATION:The objective 2-aminoxypropionic acid derivative of formula VI (hereafter Y is not H) and formula VII can be produced e.g. by carrying out the substitution reaction of a compound of formula IV with a compound of formula III derived from 3-hydroxypropionic acid derivative of formula II and deprotecting the resultant compound of formula V.

30. 发明专利

JPS6280A PRODUCTION OF PHTHALIDE COMPOUND 失效
公开(公告)号：JPS6280A
公开(公告)日：1987-01-06
申请号：JP13719085
申请日：1985-06-24
申请人： MITSUBISHI CHEM IND
发明人： TANIGUCHI SEIRO , MORITA YOSHIMI , HAYAKAWA SHUZO
IPC分类号： C07D307/88
摘要： PURPOSE:To obtain the objective compound in high yield suppressing the production of by-product, by using a specific amount of hydrochloric acid in the process for the production of a phthalide by the reaction of a trialkoxybenzoic acid with formaldehyde in the presence of hydrochloric acid. CONSTITUTION:The phthalide compound of formula III useful as an intermediate for tritoqualine (a medicine having anti-allergy action, etc.) is produced by reacting the trialkoxybenzoic acid of formula I (R -R are lower alkyl) with formaldehyde in the presence of hydrochloric acid. In the above process, the amount of the hydrochloric acid is selected to 1/100-1/200pts.wt. per 1pt. of the sum of formaldehyde and water in terms of hydrogen chloride. The by- production of 7-chloromethyl-4,5,6-trialkoxyphthalide can be suppressed and the yield of the objective compound can be improved by this process. The amount of formaldehyde is preferably 3-20mol per 1mol of the compound of formula I, and the reaction temperature is preferably 70-110 deg.C.

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