CAS: 54573-75-0; (1R,3S,Z)-5-((E)-2-((1R,3As,7Ar)-1-((2R,5R,E)-5,6-Dimethylhept-3-En-2-yl)-7A-Methylhexahydro-1H-Inden-4(2H)-Ylidene)Ethylidene)-4-Methylenecyclohexane-1,3-Diol

该化合物是维生素D2的合成仿真物,主要用于治疗二级超双甲状腺病,特别是慢性肾病患者;它作为维生素D受体激动剂,促进钙吸收并调节对硫酸激素的水平;Doxercalciferol,其特点是它能够加强对钙和磷酸盐的肠内吸收,从而推动骨骼健康和矿物代谢;该物质通常通过口服或静脉注射方式施用,这取决于临床情况;其化学结构包括一个1位的氢氧基体,它与其他维生素D化合物区别开来,并增强它的营养.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

反式-度骨化醇 1α-Hydroxy-5,6-Trans-Vitamin D2 74007-20-8
阿法骨化醇 1α-Hydroxyvitamin D3 41294-56-8
维生素d2 Calciferol 50-14-6
(1Alpha,3Beta)-胆甾-5-烯-1,3-二醇 1α,3β-Dihydroxycholest-5-Ene 26358-75-8

合成工艺路线路线简述

    维生素d2置于吡啶,叔丁基过氧化氢,Selenium(Iv) Oxide,碳酸氢钠,Potassium Hydroxide体系中,用 1,4-二氧六环,癸烷,乙醇,醋酸异丙酯 作为反应溶剂,化学反应 168.83H,反应生成 度骨化醇
    参考文献: Stabilized Doxercalciferol And Process For Manufacturing The Same[fr] Doxercalciférol Stabilisé Et Son Procédé De Fabrication
    标题: Stabilized Doxercalciferol And Process For Manufacturing The Same[fr] Doxercalciférol Stabilisé Et Son Procédé De Fabrication
    摘要:一种具有极高纯度和稳定性的1α-羟基维生素d2(多西骨化醇)是通过一种过程制备的,该过程涉及经色谱纯化的1α-羟基维生素d2单乙酰化物,从纯化产物中化学去除乙酰保护基以形成1α-羟基维生素d2,并从基本上由至少一种c1-C6二烷基醚或c1-C6烷基酯和至少一种c5-C12烃组成的混合有机溶剂中沉淀所形成的1α-羟基维生素d2.

    海关参考信息

    专利信息


    专利号:US-6844461-B2
    优先权日:2001-07-30
    标 题:Synthesis of A-ring synthon of 19-NOR-1α,25-dihydroxyvitamin D3 from (D)-glucose
    发明人:DELUCA HECTOR F; SHIMIZU MASATO; YAMADA SACHIKO
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.

    专利号:US-5089647-A
    优先权日:1989-03-09
    标题:Method for preparing intermediates for the synthesis of steroid side chains in optically active form
    发明人:DELUCA HECTOR F; SCHNOES HEINRICH K; PERLMAN KATO L
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:This invention provides a novel method for the preparation of optically active arylalykylsulfone derivatives, having a chiral center in the alkyl moiety in either the (R)- or the (S)-configuration. These optically active sulfones find use in the stereospecific synthesis of steroid or vitamin D compounds having chiral center at either carbon 24 or carbon 25 of the side chain. The method comprises the steps of reacting an optically active sulfinate ester having a chiral center at sulfur with a racemic alkyl Grignard reagent to obtain a mixture of diastereomeric sulfoxides, separating the mixture of diastereomeric sulfoxides, and oxidizing separately each of the diastereomers to obtain the desired optically active sulfone.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-9221753-B2
    优先权日:2004-02-03
    标题:Process for the synthesis of vitamin D compounds and intermediates for the synthesis of the compounds
    发明人:KASHIWAGI HIROTAKA; ONO YOSHIYUKI
    权利人:KASHIWAGI HIROTAKA; ONO YOSHIYUKI; CHUGAI PHARMACEUTICAL CO LTD
    摘要:An object of the present invention is to provide a process for synthesizing a vitamin D compound by simple procedures at lower costs. n The present invention provides a process for preparing a vitamin D compound and an intermediate thereof, comprising the step of: (a) mixing a ketone or aldehyde, a Wittig reagent, and a base; or (b) mixing a ketone or aldehyde and a Wittig reagent, and then adding a base to the resulting mixture.

    专利号:EP-1494680-B1
    优先权日:2002-03-25
    标题 :Use of carbon-2-modified-vitamin d analogs to induce the formation of new bone
    发明人:DELUCA HECTOR F; PIKE J WESLEY; SHEVDE NIRUPAMA K
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:It has been discovered that the 2-carbon-modified derivatives of 1α,25-dihydroxyvitamin D3 specifically stimulate osteoblasts to form new bone. The ability of the 2-carbon-modified vitamin D analogs to stimulate new bone formation suggest that these compounds can be used where synthesis of new bone is required. Thus, these compounds can be used either systemically or locally to stimulate the growth of bone transplants, to increase the rate of fracture healing and thereby reduce the time required for the healing of fractures, the stimulation of bone growth when required for replacement surgery, and also for the growth of bone to implants or other devices required to maintain the skeleton or teeth in the proper positions.

    专利号:US-5869472-A
    优先权日:1994-07-18
    标 题 :Synthesis of 1α-hydroxy vitamin D
    发明人:MORIARTY ROBERT M; GUO LIANG; PENMASTA RAJU A
    权利人:BONE CARE INT INC
    摘要:A method for 1α-hydroxylation of vitamin D compounds using the appropriate vitamin D as the starting material. The method requires no separatory procedures prior to the actual hydroxylation step.
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    主要参考文献


    1: Dennis VC, Albertson GL. Doxercalciferol treatment of secondary hyperparathyroidism. Ann Pharmacother. 2006 Nov;40(11):1955-65. doi: 10.1345/aph.1G523. Epub 2006 Oct 24. 20(3):244-252. doi: 10.4103/aja.aja_14_18.
    3: Gembillo G, Siligato R, Amatruda M, Conti G, Santoro D. Vitamin D and Glomerulonephritis. Medicina (Kaunas). 2021 Feb 22;57(2):186. doi: 10.3390/medicina57020186.
    4: Li J, Li N, Yan S, Liu M, Sun B, Lu Y, Shao Y. Doxercalciferol Alleviates Bone Deteriorations and Cartilage Degeneration in Aging Mice. Exp Clin Endocrinol Diabetes. 2020 Aug;128(8):540-547. doi: 10.1055/a-0754-1956. Epub 2018 Oct 31. 43(5):877-90. doi: 10.1053/j.ajkd.2004.01.012. 17(12):1051-8. doi: 10.1016/j.cardfail.2011.08.006. Epub 2011 Sep 9.

    合成参考文献


    摘要:Proceedings of the Society for Experimental Biology and Medicine., 178(432), 1985 []
    参考文献:10.1007/s00467-004-1478-0
    摘要:Cunningham J. New Vitamin D analogues for osteodystrophy in chronic kidney disease. Pediatr Nephrol. 2004 Jul;19(7):705–8. doi: 10.1007/s00467-004-1478-0.
    参考文献:10.1007/s11255-008-9346-7|10.1007/s11255-008-9389-9
    摘要:Kovesdy CP, Kalantar-Zadeh K. Bone and mineral disorders in pre-dialysis CKD. International Urology and Nephrology. 2008 Mar 27;40(2):427–40. doi: 10.1007/s11255-008-9346-7.
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