Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Merck Sharpe & Dohme Corp.

Michael Stewart Ashwood

Ian Frank Cottrell

John M Williams

Ulf H Dolling

Ronald B Jobson

Mark Cameron

David Hands

Karel M Brands

Brian Christopher Bishop

Robert Darrin Wilson

Antony J Davies

Joseph E Lynch

Guy R Humphrey

Edward Cleator

Faye Sheen

Peter G Houghton

John Simon Edwards

Cameron John Cowden

Brian Cchristopher Bishop

Guo Jie Ho

Matthew Bio

Debra Jane Wallace

Brian Christopher Bishops

Khateeta Moneek Emerson

Yao Jun Shi

A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein Rand Rare each independently hydrogen, or Calkyl groups or Rand Rare linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring. 

Process for the preparation of tetrazolytetrahydrocyclopentapyrazoles

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

Chemical synthesis of spirocyclic piperidines by double ring-closing metathesis

The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-.alpha.-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.

Chemical synthesis of a chiral 1,4-oxazin-2-one

A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.

Process for synthesizing carbapenem side chain 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

A process for preparing a single enantiomer of a 4-aryloxyazetidin-2-one derivative in optically pure form comprises reacting a hindered vinyl ester with chlorosulphonyl isocyanate; displacing the hindered acyloxy group with a phenolic derivative containing a protected carboxy group; deprotecting the carboxylate moiety; resolving with a chiral amine; filtering; and regenerating the desired enantiomer by acidification. A method for enriching the product obtained from the acyloxy displacement step in favour of the desired enantiomeric form, by treating with an asymmetric catalyst such as a chiral alkaloid derivative, is provided; as also is a method for racemising the unwanted antipode of the desired 4-aryloxyazetidin-2-one enantiomer. The invention further provides novel enantiomers based on the 4-aryloxyazetidin-2-one ring structure.

Process for the preparation of chiral 4-aryloxyazetidinones

Growing community of inventors

Bishops Stortford, United Kingdom

Michael Stewart Ashwood