Merck + Co., Inc.

Mark S Jensen

Nobuyoshi Yasuda

Chunhua Yang

Kenneth M Wells

Yi Xiao

Robert D Larsen

Lihu Yang

Changyou Zhou

John Y Chung

Daniel Richard Sidler

Nelo R Rivera

Dongwei Cai

Yaling Wang

Wenjie Li

Michael Palucki

Min Ge

Johnnie L Leazer, Jr

Fred Fleitz

Dorian Nelson

Elizabeth Szumigala

David A Colon

Scott Hoerrner

Gary Javadi

An efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl} cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt are provided. The succinate salt is crystalline and has superior properties.

CCR-2 antagonist salt

The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine 

Process for the preparation of CCR-2 antagonists

A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-&lcub;2-oxo-3-&lsqb;3-(5,6,7,8-tetrahydro-&lsqb;1,8&rsqb;naphthyridin-2-yl)-propyl&rsqb;imidazolidin-1-yl&rcub;-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists

Crystalline 2-hydroxymethyl carbapenem intermediate compounds and process for synthesis thereof

A process of synthesizing a carbapenem compound of formula 6:

Process for the synthesis of carbapenem intermediated and compounds produced

Process for synthesizing carbapenem intermediates

The present invention relates to a process for synthesizing novel intermediates of formula III: ##STR1## wherein R.sup.1 is a halogen. The intermediate compounds described herein are useful for the preparation of carbapenem compounds.

Process for the synthesis of 1-aza-5-halo-5-stannabicyclo[3.3.3]undecane

A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.

Process for the synthesis of carbapenem intermediates, and compounds

Growing community of inventors

Holmdel, NJ, United States of America

Mark S Jensen