Pyridine phenylation

Pyridine-, Phenyl-, Pyrimidine- and Pyrazole-based CB] Receptor Antagonists 295... 

PYRIDINE-, PHENYL-, PYRIMIDINE- AND PYRAZOLE-BASED CBi RECEPTOR ANTAGONISTS... 

Pyridine, butenyl Cured Lf smoke Pyridine, phenyl-3 Cured Lf ... 

Chloroformamidinium chlorides (29) are generated from DMF and oxalyl chloride in acetonitrile. After addition of the carboxylic acid the activated ester (26f) is formed and treated with a solution of the alcohol in pyridine. Phenyl, alkyl and even r-butyl esters may be prepared in yields of greater than 80% (equation 11). Reagent (31), accessible from (30) and oxalyl chloride (equation 12) behaves quite similarly to (29). The use of silyl esters (26g), which are formed in situ in Ae presence of the alcohol and react then to the esters, has already been mentioned in Section 2.2.1.2.1. An application is described in Table 1. 

A-(6-Chloronaphthalen-2-)sulfonylpiperazine derivatives 4 and 5 (Figure 15.12) are potent factor Xa inhibitors. Haginoya et al proposed to replace the pyridine-phenyl or the pyridine-piperidine residue by a fused-bicyclic ring which contains an aliphatic amine and a pyridine to yield the compound 6 that has an interesting factor Xa inhibitor activity. The bioisosteric replacement of the pyridine moiety of the 6-methyl-5,6,7,8-tetrahydro-[l,6]naphthyridine by phenyl, thiophene, or thiazole analogs yielded analogs with similar or better antifactor Xa activity, but also to conserve a moderate bioavailability. 

Hydroxypyridine 1-oxide 2-(2-Hydroxyphenyl)pyridine Phenyl(2-pyridyl)methanol 2-(l-Hydroxyethyl)pyridine... 

Oder 3)-hydnizon] 21 II375. Cinehomerona uire-die id 22,158. 3-[4-Carboxy-benzoyl]-pyridin.phenyl hydrazon 22, 318. 

PBI or poly ether of pyridine + phenyl phosphine oxide, PPyPO... 

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