Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.

Abstract: Salts that contain AA-PBZ monomer ions and BB-PBZ monomer ions can be precipitated from an aqueous solution by contacting soluble salts of the monomers in an aqueous solution. The monomer salt can be polymerized by ordinary techniques to form polybenzazole polymers without the need for devolatilization and with very accurate stoichiometric control.

Abstract: 4-Haloquinazolines can be prepared by the halogenation of the corresponding 4-hydroxyquinazolines with a phosphoryl, thionyl or carbonyl halide in the presence of a catalytically effective amount of a N,N-dialkylformamide. The reaction is catalyzed by the addition of soluble organic halide salts.

Abstract: 5-Amino-3-chlorosulfonyl-1,2,4-triazole is prepared by the chlor-oxidation of 5-amino-3-mercapto-1,2,4-triazole. The process is characterized by the preformation of disulfide from the mercaptan prior to treatment with chlorine. The 5-amino-3-chlorosulfonyl-1,2,4-triazole reaction mixture can be directly reacted with substituted anilines to prepare N-(3-(((aryl)amino)sulfonyl)-1H-1,2,4-triazol-5-yl)amines which are useful intermediates for the manufacture of herbicides.

Abstract: 5-Methyl-N-(aryl)-1,2,4-triazolo[1,5-a]-pyrimidine-2-sulfonamides are prepared by the cyclization of N -(3-(((aryl)amino)sulfonyl)-1H-1,2,4-triazol-5-yl)amines with 4-methoxy-3-butene-2-one or its synthetic equivalents in the presence of an aqueous base. By controlling the pH of the condensation between 8.5 and 10.5, by-product formation can be substantially reduced.

Abstract: In a process for making 2,6-di-tertiarybutyl-4-mercaptophenol by the Zn/acid reduction of bis (3,5-di-tertiarybutyl-4-hydroxyphenyl)polysulfide the addition of catalytic amounts of lead to the zinc reagent results in substantial improvement in the process.

Abstract: In an improved process of converting a 1,2-epoxy-2-phenylbutane or a 1,2-epoxy-2-phenylpentane to a 2-hydroxy-2-phenylbutylsulfonate, sulfamate, or halide, or the corresponding 2-hydroxy-2-phenylpentyl compound, respectively, by the reaction at about 40.degree. to 120.degree. C. in the presence of an organic solvent of the requisite epoxybutane or epoxypentane with a proton source and a nucleophile. The proton source can be a free strong acid such as a sulfonic, sulfamic acid, or hydrohalide acid, or the proton source can be derived from an equilibrium system comprising a free strong acid and weak base in equilibrium with the respective deprotonated strong acid and protonated weak base. The process is carried out in one step with reduction or avoidance of aldehyde formation by rearrangement of the epoxyalkane.

Abstract: Process for making pyridyloxyphenol by reacting under essentially anhydrous conditions in the absence of oxygen and in a polar aprotic solvent, a 2-halopyridine with hydroquinone which has been from 75 to 100 percent neutralized to the sodium or potassium salt.

Abstract: 1-Aryl-1-hydroxy-2-methylaminopropanes are rearranged from the erythro isomer to the threo isomer by the process of (1) forming the O,N-diacyl derivative of the arylpropanolamine; (2) reacting the product of step (1) with an anhydrous or substantially anhydrous protic acid (thereby forming a novel oxazolinium salt); and (3) reacting the oxazolinium salt from step (2) with an aqueous protic acid. The threo isomer of the arylpropanolamine is thus produced as an amine/acid salt. This salt can be further purified, if desired, by neutralizing the acid/amine salt with caustic isolating the free amine and reprotonating the free base in isopropanol with, for example, anhydrous HCl. This process is particularly applicable to manufacture of d-pseudoephedrine from 1-ephedrine.