新产品编号:1269273

合成路线:Condensation of 2-amino-4-iodobenzoic acid (I) with 2-chloronicotinic acid (II) in refluxing EtOH in the presence of HCl yields pyridoquinazoline acid derivative (III),which is then condensed with N,N-dimethylethylenediamine (IV) in CH2Cl2 using BOP as coupling reagent to provide (V).Reaction of 2-bromopyridine (VI) in Et2O with n-BuLi and trimethylborate,followed by treatment with EtOH and HOAc,gives 3-pyridinyl boronic acid (VII),which is finally coupled to (V) in an Na2CO3 solution via a Suzuki coupling catalyzed by Pd(PPh3)4.

合成路线:Treatment of 4-bromophthalic anhydride (I) in MeOH with NaOMe affords methyl ester (II),which is then treated with diphenylphosphoryl azide ((PhO)2PON3) in toluene,acetone/H2O to yield a mixture of regioisomers from which derivative (III) is obtained by chromatographic separation.Condensation of (III) with 2-chloronicotinic acid (IV) in refluxing EtOH in the presence of HCl yields pyridoquinazoline acid derivative (V),which is then condensed with N,N-dimethylethylenediamine (VI) in CH2Cl2 using BOP as coupling reagent to provide (VII).Reaction of 2-bromopyridine (VIII) in Et2O with n-BuLi and trimethylborate,followed by treatment with EtOH and HOAc,gives 3-pyridinyl boronic acid (IX),which is finally coupled to (VII) in an Na2CO3 solution via a Suzuki coupling catalyzed by Pd(PPh3)4.

参考文献标题:Hetero-biaryl-pyridoquinazolinone derivs.as anti-cancer agents
文献作者:Trova,M.P.; Zhang,N.(American Cyanamid Co.)
参考来源:US 5908840


合成路线:Condensation of 2-amino-4-iodobenzoic acid (I) with 2-chloronicotinic acid (II) in refluxing EtOH in the presence of HCl yields pyridoquinazoline acid derivative (III),which is then condensed with N,N-dimethylethylenediamine (IV) in CH2Cl2 using BOP as coupling reagent to provide (V).Reaction of 2-bromopyridine (VI) in Et2O with n-BuLi and trimethylborate,followed by treatment with EtOH and HOAc,gives 3-pyridinyl boronic acid (VII),which is finally coupled to (V) in an Na2CO3 solution via a Suzuki coupling catalyzed by Pd(PPh3)4.

合成路线:Treatment of 4-bromophthalic anhydride (I) in MeOH with NaOMe affords methyl ester (II),which is then treated with diphenylphosphoryl azide ((PhO)2PON3) in toluene,acetone/H2O to yield a mixture of regioisomers from which derivative (III) is obtained by chromatographic separation.Condensation of (III) with 2-chloronicotinic acid (IV) in refluxing EtOH in the presence of HCl yields pyridoquinazoline acid derivative (V),which is then condensed with N,N-dimethylethylenediamine (VI) in CH2Cl2 using BOP as coupling reagent to provide (VII).Reaction of 2-bromopyridine (VIII) in Et2O with n-BuLi and trimethylborate,followed by treatment with EtOH and HOAc,gives 3-pyridinyl boronic acid (IX),which is finally coupled to (VII) in an Na2CO3 solution via a Suzuki coupling catalyzed by Pd(PPh3)4.
参考文献标题:Hetero biarylpyridoquinazolinone derivatives as anticancer agents
文献作者:Kitchen,D.B.; Schow,S.R.; Casscles,W.T.Jr.; Discafani,C.; Trova,M.P.; Lassota,P.; Zhang,N.; Powell,D.W.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 59