CAS: 25122-41-2; (8S,9R,10S,11S,13S,14S,16S,17R)-17-(2-Chloroacetyl)-9-Fluoro-11,17-Dihydroxy-10,13,16-Trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-Dodecahydro-3H-Cyclopenta[a]Phenanthren-3-One

上下游产品

dexamethasone methanesulfonyl chloride

倍他米松置于三乙胺,Lithium Chloride体系中,用 N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 2.5H,反应生成氯倍他索
参考文献:抗炎药倍他米松磷酸钠制备新工艺的开发
标题:抗炎药倍他米松磷酸钠制备新工艺的开发
摘要:在本文中,我们报告了我们为开发一种新型和改进的抗炎类固醇活性药物成分制剂,即倍他米松磷酸钠所做的努力.从市售的倍他米松开始,合成策略包括 C21 位羟基的甲磺酸化,然后是甲磺酸酯衍生物与二叔丁基磷酸钾的关键磷酸化反应,二叔丁基磷酸酯的水解丁酯中间体在弱酸性条件下,最终成盐.开发的工艺使我们能够以 68% 的总收率在多公斤规模下获得所需的倍他米松磷酸钠 >= 99.9% HPLC 纯度.还讨论了工艺的成本效益,杂质分析和材料质量.
Doi:10.1021/acs.Oprd.2C00329

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-2024082118-A1
优先权日:2021-05-19
标 题:Topical compositions and methods of preparing the same
发明人：ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION
权利人:LANDA LABS 2012 LTD
摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.

专利号:WO-2022226312-A1
优先权日:2021-04-22
标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
发明人：KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
权利人:CLEAR CREEK BIO INC
摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

专利号:EP-1331924-B1
优先权日:2000-10-26
标题 :Use of beta-carotene and lycopene for treating ageing symptoms via the inhibition of the expression of the metalloproteinase of type 1 of the extracellular matrix
发明人：BRETON LIONEL; BAUR MARKUS
权利人:OREAL; NESTEC SA
摘要:Intimate admixtures of at least one carotenoid having provitamin A activity and at least one carotenoid devoid of provitamin A activity are well suited for treating the undesirable cutaneous signs of skin aging, in particular the determination of the skin and/or of the mucous membranes by inhibiting the activity and/or the expression of collagenases and by increasing the synthesis of collagen.

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.