2-Chloro-3-methyl-4//-pyrido

H-Pyrido[2,l-i]purine-9-carboxylic acid, 7-oxo-methyl ester, 5, 566 Pyrido[2,3-6]pyrazine, amino-nucleophilic attack, 3, 253 Pyrido[2,3-h]pyrazine, 6-chloro-reactions... 

The chloro atom of 2-[4-(6-chloronicotinoyl)benzyloxy]-3-methyl-4//-pyrido[l,2-n]pyrimidin-4-one, its 6-methyl derivative and 2-[4-(6-chlo-ronicotinoyl)benzylthio]-3-methyl-4//-pyrido[l,2-n]pyrimidin-4-one was replaced by a 4-piperidinopiperidino and 4-phenylpiperazino group with 4-piperidinopiperidine and 4-phenylpiperazine (96EUP733633). The carboxyl group of 2-[4-(4-carboxybenzoyl)benzyloxy]-3-methyl-4//-pyrido[l,2-n]pyrimidin-4-one, prepared by hydrolysis of methyl ester in DMF with 1 N NaOH, was reacted first with diethyl pyrocarbonate in DMF at room temperature and then with 4-phenylpiperazine and 4-piperidinopiperidine to give the appropriate amide derivatives (96EUP733633). 

Bromo atom of ethyl (3S)-10-bromo-3-methyl-7-oxo-2,3-dihydro-7//-pyrido[l,2,3- fe]-l,4-benzothiazine-6-carboxylate was change for hetaryl groups with tributylstannyl derivatives of heterocycles in the presence of (Ph3P)2Pd(II)Cl2 in boiling toluene (OOMIPIO). 7-Aryl-5-oxo-2,3-dihydro-5//-pyrido[l,2,3- fe]-l,4-benzothiazine-6-carboxylates, 6-carboxamides and their 1,1-dioxide derivatives were prepared from 7-chloro derivatives in the... 

Reduction of 3-benzyl-8-chloro-4-oxo-4//-pyrido[l,2- ]pyrimidine-2-carboxylate <2004W004/064741> and 2-methyl-4-oxo-4//-pyrido[l,2-tf]pyrimidine-3-carboxylate <2003T4123> with DIBAL-H afforded 2- and 3-formyl derivatives, respectively. Reduction of /V-(4-fluorobenzyl)-3-hydroxy-8-[methoxy(methyl)amino]-4-oxo-6,7,8,9-tetra-hydro-4//-pyrido[l,2- ]pyrimidine-2-carboxamide with Zn-dust in aqueous AcOH afforded the 8-methylamino derivative, which was acylated with AcOH in the presence of Hiinig s base, HOBt, and l-(3-dimethylaminopro-pyl)-3-ethylcarbodiimide-HCl <2004W004/058756>. 3-(Perhydropyrido[l,2- ]pyrimidin-2-yl)propylamine was obtained by catalytic hydrogenation of 2-(perhydropyrido[l,2- ]pyrimidin-2-yl)propionitrile over a Pt02 catalyst <2003FRP1275647>. 

In attempts to formylate the bicyclic compound 5-methyl-9-phenylhy-drazono-6,7,8,9-tetrahydro-4-oxo-4//-pyrido[l,2- z]pyrimidine 3-carboxy-late (129) with dimethylformamide-phosphoroxychloride at 90-100°C, a degenerate ring rearrangement took place, resulting in the formation of 7-(o -chloroethyl)-8-chloro-9-(A,A-dimethylaminomethylene)amino-6,7,8,9-tetrahydro-4-oxo-4H-pyrido[l,2-a]pyrimidine-3-carboxylate (131)... 

Chen P, Doweyko AM, Norris D, et al. Imidazo-quinoxahne Src-family kinase p56 inhibitors SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-l-piper-azinyl) imidazo [l,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity J Med Chem 2004 47, 4517-29. 

The surface activity characteristics of ll//-pyrido[2,l-6]quinazolin-ll-one and its 3-chloro, 2-methoxy, 8-methyl, and 2,4-dinitro derivatives were determined in 3% hydrochloric acid (85MI1). 

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