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1. 发明申请

WO1990009974A1 PROCESS FOR PREPARING ANTHRACYCLINONES 审中-公开
标题翻译：制备蒽醌的方法
公开(公告)号：WO1990009974A1
公开(公告)日：1990-09-07
申请号：PCT/EP1990000334
申请日：1990-02-28
申请人： FARMITALIA CARLO ERBA S.R.L. , CABRI, Walter , CANDIANI, Ilaria , DE BERNARDINIS, Silvia , FRANCALANCI, Franco
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07C50/38
CPC分类号： C07C46/00 , Y02P20/55 , C07C50/38
摘要： 4-Substituted anthracyclinones of general formula (I), wherein R represents a hydrogen atom or a COOR1 group in which R1 may be a hydrogen atom or an optionally substituted C1-C10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by: (i) (a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V), wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII): MLnL'm, wherein M represents a transition metal atom, L and L', which may be the same or different, each represents an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII), wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R1OH, wherein R1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR1 group; and (ii) introducing an α-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

2. 发明专利

SK278225B6 未知
公开(公告)号：SK278225B6
公开(公告)日：1996-04-03
申请号：SK95890
申请日：1990-02-28
申请人： CABRI WALTER , CANDIANI ILARIA , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO
发明人： CABRI WALTER , CANDIANI ILARIA , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO
IPC分类号： B01J31/12 , C07B61/00 , B01J27/128 , C07C46/00 , C07C49/423 , C07C49/727 , C07C50/36 , C07C50/38
摘要： METHOD FOR PREPARATION OF ANTHRACYCLINONES The preparation method of anthracyclinones of the general formula I, wherein R means group of the formula COOR1, in which R1 means a hydrogen atom or methyl, resides in following: in the first stage the 13-keto group of the 4-demethyl-3- -deoxydaunomycinone is protected by working up with the ethylene glycol; in the second stage the resultant 4-demethyl-13- -dioxolanyl-7-deoxydaunomycinone reacts with the sulphonatic agent of the formula R'-SO2-X, in which X means the halogene atom or the group of the formula -O-SO2-R' and R' means the trifluoromethyl, p-fluorophenyl or p-tolyl group; in the third stage the resultant 4-demethyl-13-dioxolanyl-7- -deoxydaunomycinone of the general formula V reacts with the nucleophilic agent of the general formula R1OH in which R1 has a meaning listed above, and with the carbon monoxyde under presence of the triethylamine and the catalitic amount of the palladium complex with chelating ligand; and in the fourth stage the resultant 4-demethyl-4-carboxyalkyl-7-deoxy-13- -dioxolanyldaunomycinone of the general formula VII reacts with the bromine solution in the carbon tetrachloride for introduction of the alpha-hydroxy group into the position 7 of the general formula VII compound, then the 13-dioxolanyl protective group is removal and, after chromatographic treatment the required pure compound of the general formula I is obtained.

3. 发明申请

WO1990004601A1 NEW 4-SUBSTITUTED ANTHRACYCLINONES AND ANTHRACYCLINE GLYCOSIDES AND THE PROCESS FOR PREPARING THEM 审中-公开
标题翻译：新的4-取代的蒽醌和蒽醌糖苷及其制备方法
公开(公告)号：WO1990004601A1
公开(公告)日：1990-05-03
申请号：PCT/EP1989001266
申请日：1989-10-24
申请人： FARMITALIA CARLO ERBA S.R.L. , CABRI, Walter , DE BERNARDINIS, Silvia , FRANCALANCI, Franco , PENCO, Sergio
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： 4-substituted anthracyclinones of formula (I), wherein R represents a straight or branched alkyl, alkenyl or alkynyl group of up to 16 carbon atoms optionally substituted by (a) an aryl group which is unsubstituted or substituted by an inert group such as an alkyl, alkoxy or nitro group; (b) an alkoxy group; (c) a trialkylsilyl group, (d) an ester group or (e) an amido group, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX), wherein R is as defined above and R1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

4. 发明专利

SK278267B6 MANUFACTURING PROCESS OF 4-DEMETHOXYDAUNOMYCINONE 未知
公开(公告)号：SK278267B6
公开(公告)日：1996-06-05
申请号：SK215289
申请日：1989-04-07
申请人： CABRI WALTER , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO , PENCO SERGIO
发明人： CABRI WALTER , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO , PENCO SERGIO
IPC分类号： B01J31/02 , C07D317/26 , B01J31/24 , C07B61/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252
摘要： 4-demetoxydaunomycinone of a formula I is manufactured as follows: 4-demethyl-13-di-oxolanyldaunomycinone is brought, under presence of N,N-di-isopropylethylamine and catalytic amount of 4-dimethylaminopyridine, into reaction with sulfonyl compound of the general formula RSO2X, in which X means the group of the formula OSO2R, wherein R represents trifluoromethyl group; resultant sulfonated 4-demethyl-13-dioxolanyldaunomycinone is forced to react in a reduction medium in presence of a catalytic amount of a compound of the general formula MLnL°m, in which M means the transition metal atom, preferably palladium or nickel, L and L', which are the same or different, mean chloride or acetate anion, or chelatingly acted monophosphine, diphosphine, phosphite or diamine molecule, preferably 1,3-diphenylphosphinpropane or 1,1'-bis(diphenylphosphin)ferrocene and n and m mean numbers of from 0 to 4, and then the protective group on the 13-oxo group of resultant 4-demetoxy-13-dioxolanyldaunomycinone is removed by treatment with trifluoroacetic acid at ambient temperature.

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