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    PROCESS FOR PREPARATION OF N-PYRIMIDINYL-IMIDO ACID ESTERS
    1.
    发明授权
    PROCESS FOR PREPARATION OF N-PYRIMIDINYL-IMIDO ACID ESTERS 失效

    公开(公告)号：KR820001321B1

    公开(公告)日：1982-07-23

    申请号：KR780002117

    申请日：1978-07-08

    Applicant: BASF AG

    Inventor： SCHARWAECHTER P ,  GUTSCHE K ,  KOHLMANN W

    IPC: A61K31/505 ,  C07D239/48

    Abstract: Title compds. (I; R1,R2,R3 = same or different H, Me, MeO, Cl; R4 = H, C1-4 alkyl; R5 = C1-6 alkyl, benzyl; R6 = C1-4 alkyl, benzyl; n = 0,1) useful as fungicides, were prepd. by reaction of II and III. Thus, 34 g II(R1,R2,R3 = MeO; R4 = H, n = o) and 97.2 g III(R5 = Me; R6 = Et) were suspended in 240 ml dimethyl formamide and 1 ml conc. HCl and stirred for 4 hr at 80-90≦̸C to give 35.2 g I(m.p., 142-144≦̸C; yield 81.5%).

    PROCESS FOR PREPARATION OF BENZYL PYRIMIDINES
    2.
    发明授权
    PROCESS FOR PREPARATION OF BENZYL PYRIMIDINES 失效

    公开(公告)号：KR820001338B1

    公开(公告)日：1982-07-28

    申请号：KR780002075

    申请日：1978-07-05

    Applicant: BASF AG

    Inventor： GUTSCHE K ,  KOHLMANN W ,  SCHARWAECHTER P

    IPC: A61K31/505 ,  C07D239/48

    Abstract: Benzyl pyrimidines(I; R1, R2,R3 = H, methyl, methoxy, Cl; R4 = C1-6 alkoxy, aryloxy, cyclohexaory or benzyloxy substituted methyl, phenyl, chlorophenyl, hydroxyl, C1-2 alkoxy, dialkylamino, 3-alkylisoxazolyl-5-methyl; Hal is halogen), having antibiotic activity, were prepd. by reacting compd. (II) with compd. (III). Thus, 2,4-diamino-5-(3,4,5- trimethoxy benzyl)-pyrimidine 5.8 g was dissolved in pyridine 60 ml at 60≦̸C, chlorodimethyl ether 3.0 ml was added and then pyridine was eliminated by distillation under reduced pressure. The residue was recrystallized with ethanol 250ml to give 2-methoxymethylamino-4-amino-5-(3,4,5-trimethoxylbanzyl)-pyrimidine HCl 15.5 g (m.p. 227≦̸C).

    PROCESS FOR PREPARATION OF AMDIDINO-BENZYLPYRIMIDINES
    3.
    发明授权
    PROCESS FOR PREPARATION OF AMDIDINO-BENZYLPYRIMIDINES 失效

    公开(公告)号：KR820001307B1

    公开(公告)日：1982-07-21

    申请号：KR780002191

    申请日：1978-07-14

    Applicant: BASF AG

    Inventor： WAECHTER P ,  GUTSCHE K ,  KOHLMANN W

    IPC: A61K31/505 ,  C07D239/48

    Abstract: Title compd. I (R1,R2,R3 = H, Me, MeO, Cl; R4 = C1-6 alkyl, benzyl; R5,R6 = H, C1-4 alkyl, benzyl, Ph, cyclohexyl, furfuryl), useful as antibiotics, were prepd. by reacting compd. II with amine(III). Thus, 16.2 g N-[4-amino-5-(3,4,5-trimethoxybenzyl)-pyrimidin-2-yl -acetamido ethyl ester was dissolved in 120 ml pyridine, inwhich 14 ml satd. ammonium soln. (dissolved in EtOH) was added and stirred at 10≦̸C for 12 hr, vacuum concentrated, and recrystallized to give 8.6g N-[4-amino-5-(3,4,5-trimethoxybenzyl) -pyrimidin -2-yl acetamidine(m.p. 207≦̸C).

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