申请人:SMITHKLINE BECKMAN CORPORATION
公开号:EP0058055A2
公开(公告)日:1982-08-18
Pyrimidinones of formula A
in which:
het is an optionally substituted, acid stable, 5 or 6 membered heteroaryl ring having at least one nitrogen ring member; Z is het'-CH2-Y-CH2CH2- or R3R4NCH2-phenyl-O-CH2CH2CH2-; het' is an optionally substituted, 5 or 6 membered heteroaryl ring; Y is CH2 or S; and R3 and R4 are lower alkyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or morpholino group; are prepared by reacting a compound of the formula B
in which:
R2 is alkyl of 1-5 carbon atoms, benzyl, allyl, phenyl, 2-methoxyethyl or 2,2,2-trichloroethyl; and het and Z are as defined above with a hydrolytic agent or also, when R2 is benzyl or allyl, by catalytic hydrogenation over a noble metal catalyst.
式 A 的嘧啶酮
其中
het 是任选取代的、酸性稳定的、5 或 6 个成员的杂芳基环,至少有一个氮环成员; Z 是 het'-CH2-Y-CH2CH2- 或 R3R4NCH2-苯基-O-CH2CH2CH2-; het' 是任选取代的、5 或 6 个成员的杂芳基环;Y 是 CH2 或 S;R3 和 R4 是低级烷基或与所连接的氮原子一起形成吡咯烷基、哌啶基或吗啉基; 通过反应式 B 的化合物制备。
其中
R2 是 1-5 个碳原子的烷基、苄基、烯丙基、苯基、2-甲氧基乙基或 2,2,2-三氯乙基;以及 het 和 Z 如上文所定义。