Abbott Laboratories Corporation

Bristol-myers Squibb Compnay

Other

Padam N Sharma

Yi-Yin Ku

Marlon D Cowart

Howard E Morton

Yu-Ming M Pu

Susan D Boettger

Saibaba Racha

Edward J Gublo

Robert J Altenbach

Lawrence A Black

Gregory A Gfesser

Youssef L Bennani

Huaqing Liu

Ramin Faghih

Kirill A Lukin

Diana L Nersesian

Sou-Jen Chang

Michael P Curtis

Timothy A Grieme

Gabriel M Galvin

Prasad S Raje

Mike A Fitzgerald

Steven A King

Daniel J Plata

John J Usher

Elaine C Lee

Ashok K Gupta

Marazban H Vandrevala

Yu-Ming Pu

Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Bicyclic-substituted amines as histamine-3 receptor ligands

Novel C-Calkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C-Calkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C-Calkyl- and aryl-thiotrifluoroacetates is also provided wherein a C-Calkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C-Calkyl- or aryl-thiotrifluoroacetate. In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a Cto Calkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.

Alkyl and aryl-thiotrifluoroacetates and process

A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reaget and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicabonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein

The invention relates to a process for preparing 2-methylpyrrolidine and, more particularly, specific enantiomers of 2-methylpyrrolidine. Novel intermediates also are described.

Process for preparing 2-methylpyrrolidine and specific enantiomers thereof

A process is provided for preparing the dipeptidyl peptidase of the structure I (also referred to as saxaglipitin)by direct dehydration, in one pot, of the amide II by reacting amide II with phosphorus oxychloride in an organic solvent such as dichloromethane, quenching the reaction mixture with water to form the hydrochloric acid salt of I, and treating the hydrochloric acid salt with base to form the free base of I.

Process for producing a dipeptidyl peptidase IV inhibitor

A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate)which is converted to acid chloride compound 5 (which is a novel compound)using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors.

Process for the preparation of cell proliferation inhibitors

The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno&lsqb;3,4-f&rsqb;quinolines.

Process for the preparation of 5-(substituted)-10 methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno &lsqb;3,4-F&rsqb; quinolines and derivatives thereof

Process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno&lsqb;3,4-F&rsqb;quinolines and derivatives thereof

The present invention relates to an improved process for the preparation of nicotinic acids represented by the following structural formula (I): ##STR1## which are prepared by reacting a nicotinic amide compound having the formula: ##STR2## under acidic conditions with a nitrite salt. In the process of the invention have the groups R.sup.1, R.sup.2, and R.sup.3, in the compounds are independently selected from the group consisting of hydrogen, and halogen atoms and R.sup.4 is selected from the group consisting of hydrogen, lower alkyl and aryl. The process provides the nicotinic acid compounds in improved yields.

Process for the preparation of nicotinic acids

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Manlius, NY, United States of America

Padam N Sharma