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1. 发明公开

EP0072200A3 Steroidal esters and process for the preparation of steroidal esters 失效
标题翻译：甾族酯和制备甾族酯的方法
公开(公告)号：EP0072200A3
公开(公告)日：1983-06-01
申请号：EP82304116
申请日：1982-08-04
申请人： PLURICHEMIE ANSTALT
发明人： Page, Philip Ronald Rua dos Girassois, Lote 38A , Heggie, William
IPC分类号： C07J05/00 , C07J07/00 , A61K31/57
CPC分类号： C07J5/0053 , C07J5/0076 , C07J7/0055 , C07J7/0085
摘要： A process for the preparation of corticosteroid esters of the formula
wherein
--- signifies that a double bond can be present; X is hydrogen, fluorine or chlorine; R 1 is hydrogen, fluorine, chlorine or methyl, which may be either a or β; R 2 is halogen, oxo, i.e. ketonic oxygen, or hydroxyl; R 3 is hydrogen, a-methyl or β-methyl; R 4 is an acyl group of the formula RCO, in which R is one of the following:
i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic; ii) an aralkyl group of 7 to 8 carbon atoms; or iii) a phenyl group; R 5 is hydroxyl or R 6 ; where R 6 is hydrogen, halogen, two halogen atom substituents or OR 7 , where R 7 is an acyl group of the formula R'CO in which R', which can be identical or different to R in the same molecule, is one of the following:
i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic; ii) an aralkyl group of 7 to 8 carbon atoms; or iii) a phenyl group;
which comprises esterifying a compound of the formula wherein X, R 1 , R 3 and R 5 are as defined above, and R 8 is trihaloacetate, halogen or oxo; at the 17-position only, or at the 17-and 21-positions when R 5 , in formula III, is hydroxyl, the said esterification being carried out with the anhydride of the acid containing the group it is desired to enter at the 17- position, or at the 17- and 21- positions, together with a pair of strong acids; and if desired eliminating immediately thereafter any 11-trihaloacetate substituent, to form a compound of formula I, wherein R 2 is hydroxyl, Rs is R 6 , and X, R 1 , R 3 and R 4 are as defined above; or when R 8 is halogen or oxo and R 5 is R 6 , isolating a compound of formula I after the said esterification; or treating a compound of formula IV from the esterification
wherein R 5 is R 6 , by eliminating the 11-trihaloacetate group therefrom by reaction, in the presence of a lower alcohol, with an organic amine (other than one in which the nitrogen forms part of an aromatic ring), or ammonia gas dissolved in a suitable anhydrous solvent, or ammonium hydroxide or hydrazine, to produce a compound of formula I wherein R 2 is hydroxyl, R 5 is R 6 and X, R 1 , R 3 and R 4 are as defined from formula I; or by so eliminating the 11-trihaloacetate group from a compound of formula
wherein X, R 1 and R 3 are as defined forformula I; R 9 is an alkyl group of 1 to 3 carbon atoms; and R 10 is a hydrocarbon group comprising one of the following:
i) an alkyl group of 1 to 16 carbon atoms, whether straight-chained, branched or cyclic; ii) an aralkyl group of7 to 8 carbon atoms; or iii) a phenyl group;
to form a compound of formula 1, wherein R 2 and R 5 are both hydroxyls, and R 1 , R 3 , R 4 and X are as defined for formula I.
摘要翻译：一种制备下式的皮质类固醇酯的方法，其中---表示可以存在双键; X是氢，氟或氯; R1是氢，氟，氯或甲基，其可以是α或β; R2是卤素，氧代即酮氧或羟基; R3是氢，α-甲基或β-甲基; R4是式RCO的酰基，其中R是以下之一：i）含有1-16个碳原子的烷基，无论是直链的，支链还是环状的; ii）7至8个碳原子的芳烷基; 或iii）苯基; R5是羟基或R6; 其中R 6是氢，卤素，两个卤素原子取代基或OR 7，其中R 7是式R'CO的酰基，其中R'可以与同一分子中的R相同或不同，为以下之一： i）含有1至16个碳原子的烷基，无论是直链，支链还是环状的; ii）7至8个碳原子的芳烷基; 或iii）苯基; 该方法包括将下式化合物酯化：其中X，R1，R3和R5如上所定义，且R8为三卤代乙酸酯，卤素或氧代; 在式III中R5是羟基时，所述酯化反应是在含有该基团的酸的酸酐的情况下进行的，所述酯的酸酐需要在17-位置处或在17-位置和21-位置处，位置，或在17位和21位，连同一对强酸; 如果需要，立即除去任何11-三卤代乙酸酯取代基，形成式I化合物，其中R2是羟基，R5是R6，且X，R1，R3和R4如上所定义; 或者当R8是卤素或氧代并且R5是R6时，在所述酯化后分离式I化合物; 或通过在低级醇存在下，用有机胺（除了其中氮形成一部分的一个有机胺的反应）除去11-三卤代乙酸酯基团，从其中R5是R6的酯化反应中处理式IV化合物芳香环）或氨气溶解于合适的无水溶剂或氢氧化铵或肼中，生成式I化合物，其中R 2为羟基，R 5为R 6且X，R 1，R 3和R 4如式I所定义; 或者通过如此从式III化合物中除去11-三卤代乙酸酯基团，其中X，R1和R3如式I所定义; R9是1至3个碳原子的烷基; 并且R 10是包含以下之一的烃基：i）具有1至16个碳原子的烷基，无论是直链的，支链的还是环状的; ii）7至8个碳原子的芳烷基; 或iii）苯基; 以形成式1的化合物，其中R 2和R 5都是羟基，且R 1，R 3，R 4和X如对式I所定义。

2. 发明授权

EP0072200B1 Steroidal esters and process for the preparation of steroidal esters 失效
标题翻译：甾族酯和制备甾族酯的方法
公开(公告)号：EP0072200B1
公开(公告)日：1985-11-21
申请号：EP82304116.5
申请日：1982-08-04
申请人： PLURICHEMIE ANSTALT
发明人： Page, Philip Ronald Rua dos Girassois, Lote 38A , Heggie, William
IPC分类号： C07J5/00 , C07J7/00 , A61K31/57
CPC分类号： C07J5/0053 , C07J5/0076 , C07J7/0055 , C07J7/0085

3. 发明公开

EP0565800A3 Process for the recovery of noble metals and tertiary phosphines 失效
标题翻译：贵金属和叔膦的回收工艺
公开(公告)号：EP0565800A3
公开(公告)日：1994-02-09
申请号：EP92311700.6
申请日：1992-12-22
申请人： PLURICHEMIE ANSTALT
发明人： de Oliveira Bandarra, Joao Jose , Ganchas de Carvalho, Alexandre Jose , Heggie, William
IPC分类号： C22B3/00 , C22B3/44 , C22B3/46 , B01J31/40 , B01J38/68 , B01J23/96
CPC分类号： C22B11/10 , C22B3/16 , Y02P10/234
摘要： The present invention concerns a process for the recovery of a noble metal from an inorganic and/or organic residue in the form of a tellurium amalgam characterised by adding a solvent having a boiling point above 120°C to the residue, removing by distillation water and other residual solvents having boiling points below the boiling point of the added solvent, adding the tellurium or reducible tellurium compound, and then refluxing at atmospheric pressure before separating the amalgam of the noble metal. The process of the present invention also allows the simultaneous recovery of the tertiary phosphine as its oxide from a residue containing a tertiary phosphine by the further stages of concentrating the mother-liquors remaining after separation of the amalgam of the noble metal, recovering the added high boiling point solvent and isolating the tertiary phosphine in the form of its oxide by precipitation with water.
摘要翻译：本发明涉及从碲汞齐形式的无机和/或有机残余物中回收贵金属的方法，其特征在于向残余物中加入沸点高于120℃的溶剂，通过蒸馏除去水和其它沸点低于添加溶剂沸点的残留溶剂，加入碲或可还原碲化合物，然后在分离汞齐贵金属之前在大气压下回流。本发明的方法还允许从含有叔膦的残余物中同时回收作为其氧化物的叔膦，进一步浓缩分离贵金属汞齐后剩余的母液，回收加入的高通过用水沉淀来分离其氧化物形式的叔膦。

4. 发明公开

EP0565800A2 Process for the recovery of noble metals and tertiary phosphines 失效
标题翻译： Verfahren zur Gewinnung von Edelmetallen undtertiärenAminen。
公开(公告)号：EP0565800A2
公开(公告)日：1993-10-20
申请号：EP92311700.6
申请日：1992-12-22
申请人： PLURICHEMIE ANSTALT
发明人： de Oliveira Bandarra, Joao Jose , Ganchas de Carvalho, Alexandre Jose , Heggie, William
IPC分类号： C22B3/00 , C22B3/44 , C22B3/46 , B01J31/40 , B01J38/68 , B01J23/96
CPC分类号： C22B11/10 , C22B3/16 , Y02P10/234
摘要： The present invention concerns a process for the recovery of a noble metal from an inorganic and/or organic residue in the form of a tellurium amalgam characterised by adding a solvent having a boiling point above 120°C to the residue, removing by distillation water and other residual solvents having boiling points below the boiling point of the added solvent, adding the tellurium or reducible tellurium compound, and then refluxing at atmospheric pressure before separating the amalgam of the noble metal.
The process of the present invention also allows the simultaneous recovery of the tertiary phosphine as its oxide from a residue containing a tertiary phosphine by the further stages of concentrating the mother-liquors remaining after separation of the amalgam of the noble metal, recovering the added high boiling point solvent and isolating the tertiary phosphine in the form of its oxide by precipitation with water.
摘要翻译：本发明涉及从碲汞齐形式的无机和/或有机残余物中回收贵金属的方法，其特征在于向残余物中加入沸点高于120℃的溶剂，通过蒸馏水除去和沸点低于添加溶剂沸点的其他残留溶剂，添加碲或可还原碲化合物，然后在大气压力下回流，然后分离出贵金属的汞齐。本发明的方法还允许从含有叔膦的残余物中同时回收作为其氧化物的叔膦，通过进一步浓缩在分离贵金属的汞齐之后留下的母液的步骤，回收添加的高沸点溶剂，并通过用水沉淀分离其氧化物形式的叔膦。

5. 发明公开

EP0072200A2 Steroidal esters and process for the preparation of steroidal esters 失效
标题翻译：类固醇酯和类固醇酯的制备方法。
公开(公告)号：EP0072200A2
公开(公告)日：1983-02-16
申请号：EP82304116.5
申请日：1982-08-04
申请人： PLURICHEMIE ANSTALT
发明人： Page, Philip Ronald Rua dos Girassois, Lote 38A , Heggie, William
IPC分类号： C07J5/00 , C07J7/00 , A61K31/57
CPC分类号： C07J5/0053 , C07J5/0076 , C07J7/0055 , C07J7/0085
摘要： A process for the preparation of corticosteroid esters of the formula
wherein

--- signifies that a double bond can be present;
X is hydrogen, fluorine or chlorine;
R 1 is hydrogen, fluorine, chlorine or methyl, which may be either a or β;
R 2 is halogen, oxo, i.e. ketonic oxygen, or hydroxyl;
R 3 is hydrogen, a-methyl or β-methyl;
R 4 is an acyl group of the formula RCO, in which R is one of the following:

i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
ii) an aralkyl group of 7 to 8 carbon atoms; or
iii) a phenyl group;

R 5 is hydroxyl or R 6 ; where
R 6 is hydrogen, halogen, two halogen atom substituents or
OR 7 , where R 7 is an acyl group of the formula R'CO in which
R', which can be identical or different to R in the same molecule, is one of the following:

i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
ii) an aralkyl group of 7 to 8 carbon atoms; or
iii) a phenyl group;

which comprises esterifying a compound of the formula
wherein X, R 1 , R 3 and R 5 are as defined above, and
R 8 is trihaloacetate, halogen or oxo;
at the 17-position only, or at the 17-and 21-positions when R 5 , in formula III, is hydroxyl, the said esterification being carried out with the anhydride of the acid containing the group it is desired to enter at the 17- position, or at the 17- and 21- positions, together with a pair of strong acids; and if desired eliminating immediately thereafter any 11-trihaloacetate substituent, to form a compound of formula I, wherein R 2 is hydroxyl, Rs is R 6 , and X, R 1 , R 3 and R 4 are as defined above; or when R 8 is halogen or oxo and R 5 is R 6 , isolating a compound of formula I after the said esterification; or treating a compound of formula IV from the esterification
wherein R 5 is R 6 , by eliminating the 11-trihaloacetate group therefrom by reaction, in the presence of a lower alcohol, with an organic amine (other than one in which the nitrogen forms part of an aromatic ring), or ammonia gas dissolved in a suitable anhydrous solvent, or ammonium hydroxide or hydrazine, to produce a compound of formula I wherein R 2 is hydroxyl, R 5 is R 6 and X, R 1 , R 3 and R 4 are as defined from formula I; or by so eliminating the 11-trihaloacetate group from a compound of formula
wherein X, R 1 and R 3 are as defined forformula I; R 9 is an alkyl group of 1 to 3 carbon atoms; and R 10 is a hydrocarbon group comprising one of the following:

i) an alkyl group of 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
ii) an aralkyl group of7 to 8 carbon atoms; or
iii) a phenyl group;

to form a compound of formula 1, wherein R 2 and R 5 are both hydroxyls, and R 1 , R 3 , R 4 and X are as defined for formula I.

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