Abstract:
PURPOSE: The production method of the pyridine-2,3-dicarboxylic derivative is safe, effective, economic and an environmental harmony. CONSTITUTION: The pyridine-2,3-dicarboxylic derivative is effectively and economically produced: as the intermediate to usefully produce the herbicide 2-(2-imidazol-2-il-) nicotinic acid, the ester, and the hydrochlorides; by containing the dangerous oxidizing method such as the nitric acid oxidation of the 2,3-dialkyl or the quinolon precursor, or the base peroxide oxidation; the common new synthesis of the pyridine-2,3-dicarboxylic rate using the oxaloacetate diester or using the metal salt thereof produced the product of low degree of purity; by using the amino alkoxy( or alkyltio) oxaloacetate diester compound as the starting material or as the intermediate.
Abstract:
3,3-Diarylpropylamine derivs. of formula (I) [R1=C1-7 trivalent aliphatic hydrocarbon or a direct bond; R2, R3=H, C1-4 alkyl or NR2R3=is 4- to 6-membered N-contg. heterocyclic ring; R4=H, halo, OH, CN, C1-4 alkoxy or C1-4 alkyl opt. substd. by one to three halo; X=- N= or -CH=; A and B are each H or together form an additional c-c bond , and their salts, ester or amide derivs. are prepd. Thus, (E,E)-II was prepd. from 2,6-di-bromopyridine, 4MeC6H4CN, Et2OCH2P(O) (OEt)2, and (2-pyrrolidinoethyl) triphenylphosphonium bromide in 5 steps. (II) has an antihistaminic PA2 of 8.6. (I) exhibit antihistamine activity for treating nasal congestion, rhinitis, urticaria, etc..