Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Cancer Research Technology Limited

Astex Therapeutics Limited

Brian Christopher Bishop

Ian Frank Cottrell

Steven Howard

Kim Louise Hirst

James Daniel Osborne

Jeffrey David St Denis

Michael Stewart Ashwood

Darren James Dixon

Jonas Calleja Priede

Matthew James Gaunt

Meenakshi Sundaram Shanmugham

David Parry-Jones

Aaron Michael Dumas

Joseph E Lynch

Charlotte Mary Griffiths-Jones

Jeremy Peter Scott

Stephen Philip Keen

David Cousin

Rhian Sara Holvey

David R Lieberman

Benjamin David Cons

David Hands

Robert Darrin Wilson

Cameron Cowden

Karel Marie Joseph Brands

Gavin William Stewart

Steven Douglas Hiscock

Antony John Davies

Peter Richard Mullens

Guo Jie Ho

David John Nash

Guillaume François Parra

Nicholas Paul Richards

Isabelle Anne Lemasson

Khateeta Moneek Emerson

Yao Jun Shi

Alan Richard Burns

The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.

Isoindolinone inhibitors of the MDM2-P53 interaction and process for making them

The present invention relates to the synthesis of intermediates for the preparation of compounds of formula (A): wherein n is 2 or 3 and various salt forms of these compounds. The compounds of formula (A) are useful as &#x3b1;&#x3bd;&#x3b2;3 receptor antagonists 

&#x3b1; v integrin receptor antagonists

The present invention is directed to the improved synthesis of compounds of formula (I) an intermediate compound which is useful in the synthesis of the anticancer agents known as PSA conjugates.

Process for preparing peptide intermediates

The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl or arylC.sub.1-4 alkyl group; and R.sup.2 is a hydrogen atom, a halogen atom, or a group selected from C.sub.1-6 alkyl, CF.sub.3 or C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.

Chemical synthesis of 1,4-oxazin-2-ones

Growing community of inventors

Harlow, United Kingdom

Brian Christopher Bishop