98902-12-6Relevant academic research and scientific papers
CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
, p. 326 - 329 (2012/04/10)
A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
Selective Monoacylation of Symmetrical Diamines via Prior Complexation with Boron
Zhang, Zhongxing,Yin, Zhiwei,Meanwell, Nicholas A.,Kadow, John F.,Wang, Tao
, p. 3399 - 3402 (2007/10/03)
(Equation presented) Pretreatment of a symmetrical primary or secondary diamine with 9-BBN prior to the addition of an acyl chloride significantly suppressed undesired diacylation, and the product of monoacylation predominated. The reactive preference is interpreted as the result of a selective deactivation of one nitrogen atom of the diamine by 9-BBN.
Synthesis and antihypertensive activity of a series of 4-amino-6,7-dimethoxyquinazoline derivatives
Manoury,Binet,Dumas,Lefevre-Borg,Cavero
, p. 19 - 25 (2007/10/02)
A series of N2-[(acylamino)alkyl]-6,7-dimethoxy-2,4-quinazolinediamines was synthesized as potential α1-adrenoceptor antagonists. When administered to spontaneously hypertensive rats at 10 mg/kg po, a number of propanediamine derivatives showed good antihypertensive activity, whereas the ethanediamine derivatives, albeit being structurally more closely related to prazosin, were devoid of this property. The most active derivative, N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- 2-furancarboxamide hydrochloride, alfuzosin, showed high selectivity for peripheral α1-postjunctional adrenoceptors. At equiactive antihypertensive doses, its effect on the pressor response to postural changes in conscious dog was less marked than that shown by prazosin. In the light of these results, alfuzosin was selected for clinical evaluation.
