Wista Laboratories Ltd.

Sarah Louise Nicoll

John Mervyn David Storey

James Peter Sinclair

Christopher Paul Larch

Colin Marshall

Scott Clunas

Michael Simpson

Steven John Kemp

Helen Sarah Gibbard

John Mervyn Storey

The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein. 

Synthesis of a thiosulfonic acid by a step of periodate mediated oxidative coupling of a thiosulfonic acid with an aniline

Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as 'diaminophenothiazinium compounds') including Methylthioninium Chloride (MTC) (also known as Methylene Blue) are provided. 

Methods of chemical synthesis of diaminophenothiazinium compounds including methylthioninium chloride (MTC)

The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds

Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as 'diaminophenothiazinium compounds') including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided. 

Growing community of inventors

Old Aberdeen, United Kingdom

Sarah Louise Nicoll