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未保护的β-溴代苯胺与苄基、烷基、芳基、烯基和杂芳基硼酸酯的铃木-宫浦交叉偶联反应。

Suzuki-Miyaura cross-coupling of unprotected -bromoanilines with benzyl, alkyl, aryl, alkenyl and heteroaromatic boronic esters.

作者信息

Lubaev Alexandra E, Marvin Christopher C, Dombrowski Amanda W, Qureshi Zafar

机构信息

Department of Chemistry and Biochemistry, Baylor University Waco Texas 76706 USA.

AbbVie, Inc. 1 N. Waukegan Road North Chicago Illinois 60064 USA

出版信息

RSC Adv. 2024 Sep 16;14(40):29184-29188. doi: 10.1039/d4ra03725a. eCollection 2024 Sep 12.

DOI:10.1039/d4ra03725a
PMID:39285872
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11403387/
Abstract

A Suzuki-Miyaura cross-coupling reaction was developed on unprotected -bromoanilines. This operationally simple reaction was developed for the diversification of glucocorticoid receptor modulators (GRMs), showed compatibility to various boronic esters featuring unique functionalities, and was demonstrated on a gram scale.

摘要

在未保护的溴代苯胺上开发了铃木-宫浦交叉偶联反应。该操作简单的反应是为糖皮质激素受体调节剂（GRM）的多样化而开发的，对具有独特功能的各种硼酸酯具有兼容性，并在克级规模上得到了验证。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/ebfdb915f54e/d4ra03725a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/ad73f5ca88e0/d4ra03725a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/5fb354fd998c/d4ra03725a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/6bdc26b16568/d4ra03725a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/ebfdb915f54e/d4ra03725a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/ad73f5ca88e0/d4ra03725a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/5fb354fd998c/d4ra03725a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/6bdc26b16568/d4ra03725a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/322d/11403387/ebfdb915f54e/d4ra03725a-f4.jpg

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本文引用的文献

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Discovery of ABBV-154, an anti-TNF Glucocorticoid Receptor Modulator Immunology Antibody-Drug Conjugate (iADC).
发现 ABBV-154，一种抗 TNF 糖皮质激素受体调节剂免疫抗体药物偶联物（iADC）。
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Optimization of Drug-Linker to Enable Long-term Storage of Antibody-Drug Conjugate for Subcutaneous Dosing.优化药物连接子以实现抗体药物偶联物的长期储存，便于皮下给药。
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Applications of palladium-catalyzed C-N cross-coupling reactions in pharmaceutical compounds.钯催化的C-N交叉偶联反应在药物化合物中的应用。
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6
Palladium-Catalyzed C-H Arylation of Unprotected Anilines: Chemo- and Regioselectivity Enabled by the Cooperating Ligand [2,2'-Bipyridin]-6(1)-one.钯催化未保护苯胺的C-H芳基化反应：由协同配体[2,2'-联吡啶]-6(1)-酮实现的化学选择性和区域选择性
ACS Catal. 2022 Dec 2;12(23):14527-14532. doi: 10.1021/acscatal.2c05206. Epub 2022 Nov 11.
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Design and Development of Glucocorticoid Receptor Modulators as Immunology Antibody-Drug Conjugate Payloads.糖皮质激素受体调节剂的设计与开发：作为免疫学抗体药物偶联物的有效载荷。
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Gold-Catalyzed Cascade Reactions of 4 H-Furo[3,2- b]indoles with Allenamides: Synthesis of Indolin-3-one Derivatives.金催化4H-呋喃并[3,2-b]吲哚与烯丙酰胺的串联反应：吲哚啉-3-酮衍生物的合成
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