The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-(1-Piperazinylcarbonyl)-1,4-benzodioxane Hydrochloride( cas:70918-74-0 ) is researched.Safety of 2-(1-Piperazinylcarbonyl)-1,4-benzodioxane Hydrochloride.Campbell, Simon F.; Davey, Michael J.; Hardstone, J. David; Lewis, Brian N.; Palmer, Michael J. published the article 《2,4-Diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-Benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as α1-adrenoceptor antagonists and antihypertensive agents》 about this compound( cas:70918-74-0 ) in Journal of Medicinal Chemistry. Keywords: alpha adrenoceptor antagonist preparation; aminobenzodioxanylcarbonylpiperazinylquinazoline preparation adrenoceptor antagonist; antihypertensive aminobenzodioxanylcarbonylpiperazinylquinazoline; aminomethoxyquinazoline antihypertensive preparation; doxazosin preparation antihypertensive activity; crystal structure methoxydimethylaminobenzodioxanylcarbonylpiperazinyl hydrochloride. Let’s learn more about this compound (cas:70918-74-0).
A series of 4-amino-2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline derivatives (e.g. I; R = H, 6-MeO, 8-MeO, 6-MeCO, 7-MeCO, etc.) was synthesized for evaluation as α-antagonists and antihypertensive agents. Thus, 4-amino-2-chloro-6,7-dimethoxyquinazoline (II) was treated with N-(1,4-benzodioxan-2-yl)piperazine (III) in refluxing BuOH to give 88% I (R = H). Most compounds displayed high (nM) binding affinity for α1-adrenoceptors with no significant activity at α2-sites. Selective antagonism of the α1-mediated vasoconstrictor effects of norepinephrine is also characteristic of the series. Structure-activity relationships for α1-adrenoceptor affinity are presented, and structural similarity between the 2,4-diamino-6,7-dimethoxyquinazoline nucleus and norepinephrine is established. An α1-receptor model is presented in which charge-reinforced hydrogen bonding is important for binding of both antagonist and agonist mols. Antihypertensive activity was evaluated after oral administration (5 mg/kg) to spontaneously hypertensive rats, and several compounds displayed similar efficacy to prazosin when assessed after 6 h.
From this literature《2,4-Diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-Benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as α1-adrenoceptor antagonists and antihypertensive agents》,we know some information about this compound(70918-74-0)Safety of 2-(1-Piperazinylcarbonyl)-1,4-benzodioxane Hydrochloride, but this is not all information, there are many literatures related to this compound(70918-74-0).
Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis