CAS: 52-76-6; (8R,9S,10R,13S,14S,17R)-17-Ethynyl-13-Methyl-2,3,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-1H-Cyclopenta[a]Phenanthren-17-Ol

该化合物是一种合成蛋白质,主要用于荷尔蒙避孕和荷尔蒙替代疗法,其特点是能够模仿天然丙酮的影响,从而影响月经循环和防止排卵.Lynestrenol是一种白色的脱白晶粉,在水中溶解性极差,但在乙醇和氯仿等有机溶剂中可溶解.其分子配方为C21H28O2,其分子重量约为312.45克/摩尔.该化合物显示出蛋白酮受体的高亲近性,这对避孕效果至关重要.Lynestrenol一般是口服的,其半衰期相对较长,允许在避孕应用中每天一次服用.副作用可能包括月经出血模式的变化,体重增加和情绪变化,类似于其他荷尔蒙疗法.与任何药物一样,用户都必须咨询保健专业人员了解其益处和潜在风险.

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CAS号68-22-4 炔诺酮 | CAS号7440-44-0 活性炭 | CAS号3646-28-4 雌甾-4-烯-17-酮 | CAS号3646-30-8 雌甾-4-烯-17-醇 | CAS号51724-44-8 6β-羟基炔诺酮 | CAS号1236-00-6 10β-羟基炔诺酮

合成工艺路线路线简述

    雌甾-4-烯-17-醇置于chromium(Vi) Oxide,硫酸,异丙醇,丙酮体系中,化学反应生成 利奈孕醇
    参考文献:De Winter Et Al.,Chemistry And Industry,1959,P. 905
    标题:De Winter Et Al.,Chemistry And Industry,1959,P. 905

    海关参考信息

    专利信息


    专利号:US-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    专利号:US-8143437-B2
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
    发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
    权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
    摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

    专利号:US-7667056-B2
    优先权日:2002-08-02
    标 题 :Process and new intermediates for the preparation of steroids with a progestogen activity
    发明人:GRISENTI PARIDE; PECORA FABIO; VERZA ELISA; LEONI MASSIMO; BOSSI LAURA
    权利人:POLI IND CHIMICA SPA
    摘要:The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).

    专利号:US-6225298-B1
    优先权日:1994-11-22
    标 题 :Compositions and methods for contraception and for treatment of benign gynecological disorders
    发明人:SPICER DARCY V; PIKE MALCOLM CECIL; DANIELS JOHN R
    权利人:BALANCE PHARMACEUTICALS INC
    摘要:Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.

    专利号:US-2005239725-A1
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof

    专利号:US-2001016578-A1
    优先权日:1997-06-18
    标 题 :Compositions and methods for contraception and for treatment of benign gynecological disorders
    发明人:SPICER DARCY V; PIKE MALCOLM CECIL; DANIELS JOHN R
    权利人:BALANCE PHARMACEUTICALS INC
    摘要:Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.
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    主要参考文献


    1: Uzan S, Denis C, Pomi V, Varin C. Double-blind trial of promegestone (R 5020) and lynestrenol in the treatment of benign breast disease. Eur J Obstet Gynecol Reprod Biol. 1992 Feb 28;43(3):219-27. doi: 10.1016/j.jsbmb.2007.09.025. Epub 2008 Feb 15. Acta Endocrinol (Copenh). 1975 Apr;78(4):791-800. doi: 10.1016/j.eplepsyres.2013.02.020. Epub 2013 Apr 6. Japanese. doi: 10.3109/13625187.2012.658925. Epub 2012 Mar 4. German. French.

    合成参考文献


    摘要:
    摘要:Sannes E et al; Arch Toxicol 52 (1): 23-33 (1983)
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