Wyeth

Celgene Corporation

Celgene Car LLC

Wyeth Holdings Corporation

Innovative Garden Products, LLC

Gregg Brian Feigelson

Ivo L Jirkovsky

Joseph Zeldis

John Fitzgerald Traverse

Anita Wai-Yin Chan

Chengmin Zhang

Alexander L Ruchelman

Warren Chew

Silvio Iera

Mohit Atul Kothare

Galina Vid

Zhixian Ding

Timothy Thomas Curran

John Hamilton Sellstedt

Henry Strong

Benjamin Cohen

Hon-Wah Man

William W Leong

Maryll Elaine Geherty

Marc Sadler Tesconi

Kelvin Hin-Yeong Yong

Hong Wen

Anita W Chan

Richard Martin Heid, Jr

Joshua Hansen

Diane H Boschelli

Weihong Zhang

Sreenivasulu Megati

Marie Georges Beauchamps

David Michael Blum

Michael J Zacuto

Karen Sutherland

William Wei-Hwa Leong

Danyang Liu

Jianxin Han

Jihong Liu

Hongfeng Liu

Rocco Petruzzelli

Chengjun Ma

Steven Zhang

Shunxiang Zhang

Michael James Williams

Benjamin M Cohen

The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.

MK2 inhibitors, synthesis thereof, and intermediates thereto

Provided herein are processes for preparing 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide.

Processes for preparing 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide

Provided are processes for the preparation of enantiomerically enriched or enantiomerically pure 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable form thereof.

Processes for the preparation of (s)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and pharmaceutically acceptable forms thereof

Processes for the preparation of (S)-3-(4- (4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and pharmaceutically acceptable forms thereof

Provided herein are processes for preparing an isoindoline-1,3-dione compound, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof.

Processes for preparing isoindoline-1,3-dione compounds

Rake

This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2&#x3b8; angles (&#xb0;) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109&#xb0; C. to about 115&#xb0; C.

Crystalline forms of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile and methods of preparing the same

The present invention relates to methods for synthesizing compounds useful as 5HTagonists or partial agonists, derivatives thereof, and to intermediates thereto.

Diazepinoquinolines, synthesis thereof, and intermediates thereto

A process for making a compound of the formula comprising dialkylating a benzodioxane aniline 

Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines

This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

Process for preparation of 4-amino-3-quinolinecarbonitriles

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders. The intermediate compounds of Formula II and IV as set forth herein are also included.

Process for making chiral 1,4-disubstituted piperazines

Methods of preparing compounds of Formula I are provided.

Process for the synthesis of derivatives of 2,3-dihydro-1,4-dioxino-[2,3-f] quinoline

A process for formation of N-aryl piperazines with chiral N'-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor. In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N, N&#x2032; disubstituted piperazines act on the central nervous system at 5HT receptors.

Process for synthesizing N-aryl piperazines with chiral N'-1-[benzoyl(2-pyridyl)amino]-2-propane substitution

Growing community of inventors

Monsey, NY, United States of America

Gregg Brian Feigelson