56414-67-6Relevant academic research and scientific papers
Carboxamidation of carboxylic acids with 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI) without bases
Saito, Yukako,Ouchi, Hidekazu,Takahata, Hiroki
, p. 11129 - 11135 (2008)
Formation of carboxamides of a variety of carboxylic acids with the coupling reagent BBDI is described. This procedure permits a one pot and simple operation without the need of any bases and no base was?required for even use of amine hydrochlorides. In addition, an approach to BBDI-catalyzed carboxamidation is examined.
Potential Thyroliberin Affinity Labels. 1. Chloroacetyl-Substituted Phenylalanylpyrrolidines
Goebel, Richard J.,Currie, Bruce L.,Bowers, Cyril Y.
, p. 366 - 370 (2007/10/02)
Six analogues of thyroliberin (THR) that have a chloroacetyl substituent at the amino terminus have been prepared as potential affinity labels for the TRH receptor.These compounds are N-(chloroacetyl)-L-alanyl-L-phenylalanylpyrrolidine (ClAc-Ala-Phe-Pyrr; 14), N--L-phenylalanyl>pyrrolidine (m-ClAcBz-Phe-Pyrr; 11a), N--L-alanyl-L-phenylalanylpyrrolidine (m-ClAcBz-Ala-Phe-Pyrr; 15a), N--L-phenylalanylpyrrolidine (p-ClAcBz-Phe-Pyrr; 11b), and N--L-alanyl-L-phenylalanylpyrrolidine (p-ClAcBz-Ala-Phe-Pyrr; 15b).Pyroglutamyl-L-phenylalanylpyrrolidine was also synthesized as a model agonist.Weak agonist activity was observed for 11a, 11b, and 15b.These three analogues do not contain the amide group of the pyroglutamyl moiety that was previously thought to be essential for intrinsic activity.No significant antagonist activity was observed for these compounds at the doses tested.
