http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2339639-C2

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filingDate 2004-07-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2008-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dcbbe328a4e4565f5e342a0388eab897
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_68e840a76ba2689c78561d4676623f91
publicationDate 2008-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2339639-C2
titleOfInvention Regioselective cci-779 synthesis
abstract FIELD: chemistry. n SUBSTANCE: regioselective synthesis of complex rapamycin 42-ether (CCI-779) involves: (a) acylation of 31-silyl rapamycin ether by compound of formula HOOC.CR 7 R 8 R 9 or its combined anhydride, where: R 7 is hydrogen, alkyl with 1-6 carbon atoms, alkenyl with 2-7 carbon atoms, alkinyl with 2-7 carbon atoms, -(CR 12 R 13 ) f OR 10 , -CF 3 , -F or -CO 2 R 10 ; R 10 is hydrogen, alkyl with 1-6 carbon atoms, alkenyl with 2-7 carbon atoms, alkinyl with 2-7 carbon atoms, triphenylmethyl, benzyl, alcoxymethyl with 2-7 carbon atoms, chloroethyl or tetrahydropyranyl; R 8 and R 9 together form X; X is 2-phenyl-1,3,2-dioxaborinane-5-yl or 2-phenyl-1,3,2-dioxaborinane-4-yl, where phenyl can be optionally substituted; R 12 and R 13 each is independently hydrogen, alkyl with 1-6 carbon atoms, alkenyl with 2-7 carbon atoms, alkinyl with 2-7 carbon atoms, trifluormethyl or -F; and f=0-6; to obtain 42-ether boronate of 31-silyl rapamycin ether; (b) selective hydrolysis of 42-ether boronate of 31-silyl rapamycin ether in moderately acid environment to obtain rapamycin 42-ether boronate; and (c) diol treatment of rapamycin 42-etherboronate to obtain complex rapamycine 42-ether. Invention also claims new intermediate products applicable in this method. n EFFECT: application as antitumour medication. n 48 cl, 3 ex
priorityDate 2003-08-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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