http://rdf.ncbi.nlm.nih.gov/pubchem/patent/PL-213967-B1

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filingDate 2003-04-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ee0a9e8ed48a9c2cecc1f40e66ff7bd
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publicationDate 2013-05-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber PL-213967-B1
titleOfInvention Production method of combrestins and an indirect compound
abstract Preparation of combrestatins (I) by a Wittig condensation of (3,4,5-trimethoxybenzyl) triphenyl phosphonium bromide or chloride with 3-nitro-4-methoxy benzaldehyde, or of 3,4,5-trimethoxy benzaldehyde with a (4-methoxy-3-nitrobenzyl) triphenyl phosphonium salt, followed by reduction of the nitro group on the product in the presence of iron. Preparation of combrestatins (I) by a Wittig condensation of (3,4,5-trimethoxybenzyl) triphenyl phosphonium bromide or chloride with 3-nitro-4-methoxy benzaldehyde, or of 3,4,5-trimethoxy benzaldehyde with a (4-methoxy-3-nitrobenzyl) triphenyl phosphonium salt, followed by reduction of the nitro group on the product in the presence of iron. [Image] A' : an amino group. Independent claims are included for (1) the process as described but in which the nitro group in the starting material is replaced by an amino group; (2) preparation of 2-amino-3-hydroxy-N-{2-methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenyl}-propionamide hydrochloride salt of formula (IV) by reacting (I; A = NH 2) with a protected cyclic derivative of serine of formula (IIb), to give an intermediate (III) followed by removal of the protecting group PG; (3) intermediates of formula (III). [Image] [Image] PG : a protecting group such as tert. butoxycarbonyl, benzyloxy carbonyl, or 9-fluorenylmethyloxy carbonyl. ACTIVITY : Cytostatic. MECHANISM OF ACTION : Not given in source material.
priorityDate 2002-04-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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