专利号:US-6610844-B2 优先权日:1996-12-11 标题:Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 发明人:NG JOHN S; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; WIECZOREK JOSEPH; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; WANG PING T; YONAN EDWARD E; WEIER RICHARD M; KOWAR THOMAS R; BAEZ JULIO A; ERB BERNHARD 权利人:SEARLE & CO 摘要:Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein-A-A- represents the group -CHR4-CHR5- or -CR4=CR5-;R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano and aryloxy;R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;-B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group:where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; andR8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.
专利号:US-7129345-B2 优先权日:1995-12-11 标题:Keto-substituted steroid compounds 发明人:NG JOHN S; WANG PING T; BAEZ JULIO A; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; ERB BERNHARD; WIECZOREK JOSEPH; MUCCIARIELLO GENNARO; VANZANELLA FORTUNATO; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; YONAN EDWARD E 权利人:PHARMACIA CORP 摘要:Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.
参考标题:Processes For Preparation Of 3-Keto-7Alpha-Alkoxycarbonyl-Delta-4,5- Steroids And Intermediates Useful Therein 摘要:Multiple Novel Reaction Schemes, Novel Process Steps And Novel Intermediates Are Provided For The Synthesis Of Epoxymexrenone And Other Compounds Of Formula I Wherein:-A-A- Represents The Group -Chr4-Chr5- Or -Cr4=cr5- R3, R4 And R5 Are Independently Selected From The Group Consisting Of Hydrogen, Halo, Hydroxy, Lower Alkyl, Lower Alkoxy, Hydroxyalkyl, Alkoxyalkyl, Hydroxycarbonyl, Cyano, Varyloxy;R1 Represents An Alpha-Oriented Lower Alkoxycarbonyl Or Hydroxyalkyl Radical;-B-B- Represents The Group -Chr6-Chr7- Or An Alpha- Or Beta- Oriented Group: Where R6 And R7 Are Independently Selected From The Group Consisting Of Hydrogen, Halo, Lower Alkoxy, Acyl, Hydroxyalkyl, Alkoxyalkyl, Hydroxycarbonyl, Alkyl, Alkoxycarbonyl, Acyloxyalkyl, Cyano And Aryloxy; Andr8 And R9 Are Independently Selected From The Group Consisting Of Hydrogen, Hydroxy, Halo, Lower Alkoxy, Acyl, Hydroxyalkyl, Alkoxyalkyl, Hydroxycarbonyl, Alkyl, Alkoxycarbonyl, Acyloxyalkyl, Cyano And Aryloxy, Or R8 And R9 Together Comprise A Carbocyclic Or Heterocyclic Ring Structure, Or R8 Or R9 Together With R6 Or R7 Comprise A Carbocyclic Or Heterocyclic Ring Structure Fused To The Pentacyclic D Ring.