- Lithium tert-butoxide-mediated carboxylation reactions of unprotected indoles and pyrroles with carbon dioxide
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Unprotected indoles and pyrroles were found to undergo base-mediated carboxylation reactions under ambient pressure of carbon dioxide. It was found that this transition metal-free carboxylation reaction proceeded smoothly with the use of a large excess of LiOtBu.
- Yoo, Woo-Jin,Nguyen, Thanh V. Q.,Guiteras Capdevila, Montse,Kobayashi, Shu
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p. 1196 - 1204
(2015/04/21)
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- Base-mediated carboxylation of unprotected indole derivatives with carbon dioxide
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A simple and straightforward method for the preparation of indole-3-carboxylic acids was discovered through the direct carboxylation of indoles with atmospheric pressure of carbon dioxide (CO2) under basic conditions. The key for the reaction was found to be the use of a large excess of LiOtBu as a base to suppress the undesired decarboxylation side reaction.
- Yoo, Woo-Jin,Capdevila, Montse Guiteras,Du, Xiangwei,Kobayashi, Shu
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supporting information
p. 5326 - 5329,4
(2020/09/02)
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- Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
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The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
- Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
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p. 2843 - 2857
(2007/10/03)
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- Platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists derived from amidinoindoles
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A series of substituted amidinoindoles have been prepared as mimics of the RGD sequence and were studied as antagonists of the platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa). The agents were potent and selective antagonists of GPIIb-IIIa. Compared to their acyclic counterparts, the amidinoindole series bound with 10- to 20-fold greater affinity, indicating the advantages of added conformational restriction and/or hydrophobicity in the basic region of RGD mimics.
- Sall, Daniel J.,Arfsten, Ann E.,Berry, Dennis R.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Ray, Judith K.,Scarborough, Robert M.,Um, Suzane L.,Utterback, Barbara G.,Jakubowski, Joseph A.
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