C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 66/02 (2006.01) A61K 31/165 (2006.01) A61K 31/19 (2006.01) A61K 31/235 (2006.01) C07C 69/95 (2006.01) C07C 225/34 (2006.01) C07C 229/66 (2006.01) C07C 233/54 (2006.01) C07C 233/81 (2006.01) C07C 235/84 (2006.01) C07C 237/28 (2006.01) C07C 245/20 (2006.01) C07C 327/16 (2006.01) C07C 327/26 (2006.01) A61K 7/00 (1995.01)
Patent
CA 2211939
A process to produce rhein derivatives of formula (I). Image wherein R a is H, acyl, alkyl or aromatic group. The process is characterised by the formation of a protected diphenylketone by reaction of compounds of formula (IX) and (X), where R1-4 and Hal are defined in the specification. Image Said protected diphenylketone is treated with a strong base and then with an alkyl- or aromatic alcohol/amide/mercaptan; the resulting product is treated with a strong concentrated acid, followed by treatment with a diazotising agent and with a strong acid in aqueous medium; the resulting product is deprotected and, when R a in formula (I) is acyl, suitably acylated. The process allows to obtain highly pure derivatives of formula (1), being in particular totally free from aloe-emodin.
Laboratoire Medidom S.a.
Ridout & Maybee Llp
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