📜1-氯-3-[1-(4-甲基苯基)磺酰基-4-吲哚氧基]-2-丙醇置于sodium Hydroxide,Lithium Iodide体系中,用 乙醇 用作溶剂,化学反应 36.0H,反应生成吲哚洛尔 参考文献:Preparation Of Alkyl-Substituted Indoles In The Benzene Portion. Part 7. Synthesis Of (.+-.)-And (S)-(-)-Pindolol. 标题:Preparation Of Alkyl-Substituted Indoles In The Benzene Portion. Part 7. Synthesis Of (.+-.)-And (S)-(-)-Pindolol. 摘要:描述了一种新的短步合成β-肾上腺素能阻断剂心得安(1-(4-吲哚氧基)-3-(2-丙胺基)-2-丙醇)的方法.在酸催化下,4-[1-(4-甲基苯基)磺酰-3-吡咯基]-4-氧丁醛(14)与(+/-)-3-氯-1,2-丙二醇(12)和(R)-1-O-[(4-甲基苯基)磺酰]甘油(24)反应,得到(+/-)-1-氯-3-[1-(4-甲基苯基)磺酰-4-吲哚氧基]-2-丙醇(15)和(R)-(-)-3-[1-(4-甲基苯基)磺酰-4-吲哚氧基]-1-[(4-甲基苯基)磺酰氧基]-2-丙醇(25).这些化合物与异丙胺反应并除去吲哚氮上的保护基团,得到了(+/-)-和(S)-(-)-心得安(3和4),从而构成了从 Readily Available Aldehyde (14)出发的高效三步合成的3和4的合成方法. Doi:10.1248/cpb.40.2353
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-8026375-B2 优先权日:2007-04-13 标题:Transition metal catalyzed synthesis of N-aminoindoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE 权利人:SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
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合成参考文献
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