646515-19-7Relevant academic research and scientific papers
Development of scalable manufacturing routes to AZD1981. Application of the Semmler-Wolff aromatisation for synthesis of the indole-4-amide Core
Sulur, Manjunatha,Sharma, Parhalad,Ramakrishnan, Ravi,Naidu, Ravi,Merifield, Eric,Gill, Duncan M.,Clarke, Adrian M.,Thomson, Colin,Butters, Michael,Bachu, Sreekanth,Benison, Colin H.,Dokka, Nagaraju,Fong, Emily R.,Hose, David R. J.,Howell, Gareth P.,Mobberley, Siobhan E.,Morton, Simon C.,Mullen, Alexander K.,Rapai, Jayan,Tejas, Bharathi
, p. 1746 - 1753 (2013/01/15)
A safe and efficient synthesis of AZD1981 is described in which the indole 4-amide core is formed by a Semmler-Wolff aromatisation of a cyclohexenone oxime fused to a pyrrole ring. The substrate was obtained via Paal-Knorr pyrrole synthesis, followed by i
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981
Luker, Tim,Bonnert, Roger,Brough, Steve,Cook, Anthony R.,Dickinson, Mark R.,Dougall, Iain,Logan, Chris,Mohammeda, Rukhsana T.,Paine, Stuart,Sanganee, Hitesh J.,Sargent, Carol,Schmidt, Jerzy A.,Teague, Simon,Thom, Stephen
scheme or table, p. 6288 - 6292 (2011/11/29)
Novel indole-3-thio-, 3-sulfonyl- and 3-oxy-aryl-1-acetic acids are reported which are potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). Optimization required maintenance of high
INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF 4- (ACETYLAMINO) ) -3- [ (4-CHLORO-PHENYL) THIO] -2-METHYL-1H-INDOLE-1-ACETIC ACID
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, (2011/02/24)
The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound of formula (I): X is =0, =N-0H or =N-OC(O)Me; Y is hydrogen, PhS- or p-ch
NOVEL PROCESS
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Page/Page column 11, (2008/06/13)
The invention relates to a novel process for the preparation of substituted indoles which are useful as therapeutic agents.
INDOLE-3-SULPHUR DERIVATIVES
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Page 40, (2008/06/13)
The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. (I)
NOVEL SUBSTITUTED 3-SULFUR INDOLES
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Page 26, (2008/06/13)
The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.
