申请人:Southern Research Institute
公开号:US04526964A1
公开(公告)日:1985-07-02
There is disclosed a novel intermediate useful in the preparation of pyrido [2,3-d] pyrimidines, which includes N-[4-[(2-amino-4(3H)-oxopyrido[2,3-d]pyrimidin-6-yl)methylamino]benzoyl]-L -glutamic acid (5-deazafolic acid), N-[4-[[2-amino-4(3H)-oxopyrido[2,3-d]-pyrimidin-6-yl)methyl]methylamino]be nzoyl]-L-glutamic acid (5-deaza-N.sup.10 -methylfolic acid), N-(4-[(2,4-diaminopyrido[2,3-d]pyrimidin-6-yl)methylamino]benzoyl]-L-gluta mic acid (5-deazaaminopterin), and N-[4-[[2,4-diaminopyrido[2,3-d]pyrimidin-6-yl)methyl]methylamino]benzoyl]- L-glutamic acid (5-deazamethotrexate). This intermediate is the compound 2,4-diamino-6-(hydroxymethyl)pyrido-[2,3-d]pyrimidine.
本发明揭示了一种在制备吡啶并[2,3-d]嘧啶类化合物中有用的新型中间体,包括N-[4-[(2-氨基-4(3H)-氧代吡啶[2,3-d]嘧啶-6-基)甲基氨基]苯甲酰基]-L-谷氨酸(5-去氧叶酸)、N-[4-[[2-氨基-4(3H)-氧代吡啶[2,3-d]嘧啶-6-基)甲基]甲基氨基]苯甲酰基]-L-谷氨酸(5-去氧-N.sup.10-甲基叶酸)、N-(4-[(2,4-二氨基吡啶[2,3-d]嘧啶-6-基)甲基氨基]苯甲酰基)-L-谷氨酸(5-去氧氨基喹噁啉)和N-[4-[[2,4-二氨基吡啶[2,3-d]嘧啶-6-基)甲基]甲基氨基]苯甲酰基]-L-谷氨酸(5-去氧甲氧苯磺酸甲氨蝶呤)。该中间体是化合物2,4-二氨基-6-(羟甲基)吡啶[2,3-d]嘧啶。