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Gestrinone, A-46745, Ru-2323, R-2323, Dimetrose, Nemestran, Dimetriose

孕三烯酮Chemical Name: (17alpha)-13-Ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one; 13beta-Ethyl-17beta-hydroxy-17alpha-ethynylgona-4,9,11-trien-3-one
CAS No. 16320-04-0
项目整合开发状态: Launched-1987
项目研究机构: Aventis Pharma (Originator), Pfizer (Licensee)
合成路线:Compound can be prepared in two different ways:1) By dehydration of 13beta-ethyl-11beta,17beta-dihydroxy-17alpha-ethynyl-gona-4,9-diene-3-one (IV) with 60% formic acid at 100 C or with perchloric acid in methylene chloride containing acetonitrile.2) The ketalization of 13beta-ethyl-gona-4,9,11-triene-3,17-dione (I) by means of glycol (A) and oxalic acid in dichloroethane affords 3-ethylenedioxy-13beta-ethyl-gona-4,9,11-trien-17-one (II),which is then treated with methylmagnesium bromide (B) and acetylene (C) in THF to yield 3-ethylenedioxy-13beta-ethyl-17beta-hydroxy-17alpha-ethynyl-gona-4,9,11-triene (III).Finally,this compound is hydrolyzed in an acidic medium.
📌 参考资料/链接:
参考文献标题:R-2323
文献作者:Castar,J.; Thorpe,P.
参考来源:Drugs Fut 1977,2(2),131

📄 详细内容


合成路线:Compound can be prepared in two different ways:1) By dehydration of 13beta-ethyl-11beta,17beta-dihydroxy-17alpha-ethynyl-gona-4,9-diene-3-one (IV) with 60% formic acid at 100 C or with perchloric acid in methylene chloride containing acetonitrile.2) The ketalization of 13beta-ethyl-gona-4,9,11-triene-3,17-dione (I) by means of glycol (A) and oxalic acid in dichloroethane affords 3-ethylenedioxy-13beta-ethyl-gona-4,9,11-trien-17-one (II),which is then treated with methylmagnesium bromide (B) and acetylene (C) in THF to yield 3-ethylenedioxy-13beta-ethyl-17beta-hydroxy-17alpha-ethynyl-gona-4,9,11-triene (III).Finally,this compound is hydrolyzed in an acidic medium.

参考文献标题:19-Nor-delta(4,9,11)-gonatriene-3-ones
文献作者:Bertin,D.; Pierdet,A.
参考来源:DE 1618810; FR 1503984; GB 1128787; US 3484462


合成路线:Compound can be prepared in two different ways:1) By dehydration of 13beta-ethyl-11beta,17beta-dihydroxy-17alpha-ethynyl-gona-4,9-diene-3-one (IV) with 60% formic acid at 100 C or with perchloric acid in methylene chloride containing acetonitrile.2) The ketalization of 13beta-ethyl-gona-4,9,11-triene-3,17-dione (I) by means of glycol (A) and oxalic acid in dichloroethane affords 3-ethylenedioxy-13beta-ethyl-gona-4,9,11-trien-17-one (II),which is then treated with methylmagnesium bromide (B) and acetylene (C) in THF to yield 3-ethylenedioxy-13beta-ethyl-17beta-hydroxy-17alpha-ethynyl-gona-4,9,11-triene (III).Finally,this compound is hydrolyzed in an acidic medium.

参考文献标题:Process for the preparation of unsaturated 19-nor steroids
文献作者:Bertin,D.; Pierdet,A.
参考来源:DE 1618815; FR 1479352; GB 1128788; US 3478067


合成路线:Compound can be prepared in two different ways:1) By dehydration of 13beta-ethyl-11beta,17beta-dihydroxy-17alpha-ethynyl-gona-4,9-diene-3-one (IV) with 60% formic acid at 100 C or with perchloric acid in methylene chloride containing acetonitrile.2) The ketalization of 13beta-ethyl-gona-4,9,11-triene-3,17-dione (I) by means of glycol (A) and oxalic acid in dichloroethane affords 3-ethylenedioxy-13beta-ethyl-gona-4,9,11-trien-17-one (II),which is then treated with methylmagnesium bromide (B) and acetylene (C) in THF to yield 3-ethylenedioxy-13beta-ethyl-17beta-hydroxy-17alpha-ethynyl-gona-4,9,11-triene (III).Finally,this compound is hydrolyzed in an acidic medium.

参考文献标题:New Steroid compounds,compositions incorporating them and processes for their preparation
文献作者:Nomine,G.; et al.
参考来源:GB 1069709


合成路线:Compound can be prepared in two different ways:1) By dehydration of 13beta-ethyl-11beta,17beta-dihydroxy-17alpha-ethynyl-gona-4,9-diene-3-one (IV) with 60% formic acid at 100 C or with perchloric acid in methylene chloride containing acetonitrile.2) The ketalization of 13beta-ethyl-gona-4,9,11-triene-3,17-dione (I) by means of glycol (A) and oxalic acid in dichloroethane affords 3-ethylenedioxy-13beta-ethyl-gona-4,9,11-trien-17-one (II),which is then treated with methylmagnesium bromide (B) and acetylene (C) in THF to yield 3-ethylenedioxy-13beta-ethyl-17beta-hydroxy-17alpha-ethynyl-gona-4,9,11-triene (III).Finally,this compound is hydrolyzed in an acidic medium.
参考文献标题:Novel 13beta-alkyl-4,9,11-gonatriene-3-ones
文献作者:Nomine,G.; et al.
参考来源:DE 1291337; DE 1593307; FR 1426077; FR 1453214; FR 1492782; NL 6607609; US 3248294; US 3257278


产品链接: CAS No. 16320-04-0››