103238-56-8Relevant academic research and scientific papers
4-hydroxyindole derivatives, the process for preparation thereof and their use
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, (2008/06/13)
The invention relates to new 4-hydroxyindole derivatives of general formula: STR1 in which R represents a labile protective group and R1 can represent hydrogen, a C1 -C6 alkyl radical, a C3 -C6 cycloalkyl radical, a lower alkoxy radical, a lower hydroxyalkyl radical, a lower (lower alkoxy) alkyl radical, a phenyl radical optionally substituted with a halogen atom or a lower alkyl or lower alkoxy radical, a cyano radical, a radical of formula STR2 in which R2 and R3, which may be identical or different, each represent hydrogen or a lower alkyl radical, R4 represents a hydroxy group, a lower alkyl or lower alkoxy radical or a radical STR3 in which R2 and R3 have the same meaning as above, R5 represents a lower alkyl radical and Alk represents a single bond or a straight- or branched-chain alkylene radical having from 1 to 4 carbon atoms. The invention also relates to a process for preparing 4-(3-amino-2-hydroxypropoxy)indole derivatives from the said 4-hydroxyindole derivatives.
Process for the stereospecific synthesis of indole derivatives
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, (2008/06/13)
The present invention relates to a process for the stereo-specific synthesis of indole derivatives of formula: STR1 which consists in using 3-tosyloxy-1,2-O-isopropylidenepropane-1,2-diol (II) in an optically pure form in order to introduce the asymetric carbon C* of compound (I). Compound (II) is condensed with a suitable primary amine in order to prepare an oxazolidinone and condensation with a suitable phenol, and the oxazolidinone ring is then opened to form an indole compound (I).
