Glaxo Group Limited

Zeneca Limited

Glaxo Wellcome Inc.

Astra Zeneca U.k. Limited

Rajnikant Patel

Keith Biggadike

Diane Mary Coe

Panayiotis Alexandrou Procopiou

Brian Edgar Looker

Stephen Barry Guntrip

Dean David Edney

Michael John Monteith

Rebecca Jane Moore

Abigail Halton

Donald Lloyd Burford

Amrik Singh Mahal

The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Methods using phenethanolamine derivatives for treatment of respiratory diseases

Phenethanolamine derivatives for treatment of respiratory diseases

The present invention provides an improved (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone product which is prepared by a method which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.

One post synthesis of 2-oxazolidinone derivatives

The invention provides an improved process for preparing compounds of formula (I)

One pot synthesis of 2-oxazolidinone derivatives

The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VIl) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.

Process for preparing N.sup.G -monoalkyl-L-arginine and related compounds

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Dartford, United Kingdom

Rajnikant Patel