1-[4-(2-Azepan-1-Yl-Ethoxy)Benzyl]-5-Benzyloxy-2-(4-Benzyloxyphenyl)-3-Methyl-1H-Indole置于10 Wt% Pd(Oh)2 On Carbon Ammonium Formate体系中,用 丙酮 用作溶剂,以85%的收率获得1-[[4-[2-(氮杂环庚烷-1-基)乙氧基]苯基]甲基]-2-(4-羟基苯基)-3-甲基-吲哚-5-醇 参考文献:Processes For The Synthesis Of Bazedoxifene Acetate And Intermediates Thereof 标题:Processes For The Synthesis Of Bazedoxifene Acetate And Intermediates Thereof 摘要:高效合成药用化合物的过程,如(1-[4-(2-Azepan-1-Yl-Ethoxy)-Benzyl]-2-(4-Hydroxy-Phenyl)-3-Methyl-1H-Indol-5-Ol 醋酸,通常称为bazedoxifene 醋酸盐(化学式 Ix),使用公式 Iii 中的氰甲氧基苄卤代物,其中 X=卤素,如 Cl,F,Br,I;G=任何电子给体或电子受体取代基.
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-2012253038-A1 优先权日:2009-04-13 标 题:Processes for the synthesis of bazedoxifene acetate and intermediates thereof 发明人:JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK 权利人:JOSHI SHREERANG; BHUTA SACHIN; TALUKDAR SANJAY; SAWANT SUDHIR; VENKATRAMAN DEEPAK; SANDOZ AG 摘要:Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.
专利号:US-8828984-B2 优先权日:2012-11-19 标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection 发明人:CHE CHI MING; ZOU TAOTAO 权利人:UNIV HONG KONG; UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.
专利号:US-10577387-B1 优先权日:2018-08-09 标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment 发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng 权利人:UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
专利号:US-11286271-B2 优先权日:2018-07-31 标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment 发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG 权利人:UNIV HONG KONG 摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
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合成参考文献
参考文献:10.2147/cia.s15711 摘要:Kawate H, Takayanagi R. Efficacy and safety of bazedoxifene for postmenopausal osteoporosis. Clin Interv Aging. 2011;6():151–60. 参考文献:10.1007/s00198-011-1691-1 摘要:Silverman SL, Chines AA, Kendler DL, Kung AWC, Teglbjærg CS, Felsenberg D, Mairon N, Constantine GD, Adachi JD, for the Bazedoxifene Study Group. Sustained efficacy and safety of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled study. Osteoporosis International. 2011 Jul 21;23(1):351–63. doi: 10.1007/s00198-011-1691-1.