Accession Number : ADD012607

Title :   Pharmacological Active Amine-Carboxyboranes.

Descriptive Note : Patent Application,

Corporate Author : DEPARTMENT OF THE ARMY WASHINGTON DC

Personal Author(s) : Spielvogel,Bernard G ; McPhail,Andrew T ; Hall,Iris H

Report Date : 17 Jul 1986

Pagination or Media Count : 22

Abstract : This patent application discloses amine-carboxyborane compounds which exhibit significant antihyperlipidemic (cholesterol and/or triglyceride lowering) and antitumor activity. Amine-carboxyboranes depicted by the chemical formula R1R2NHH2BC(O)OH wherein R1 and R2 are selected from the group consisting essentially of hydrogen, methyl, ethyl, propyl, i-propyl, t-butyl, sec-butyl, and n-butyl, or when R1 is methyl, or hydrogen then R2 can be alkyl group selected from the group consisting essentially of methyl, ethyl, n-propyl, i-propyl, n-butyl, t-butyl, sec-butyl, pentyl, hexyl, octyl, nonyl, decyl, undecyl, dodecyl, trideyl, tetradecyl, pentadecyl, hexadecyl and octadecyl have been shown to exhibit significant antihyperlipidemic and antitymor activity. The process for the preparation by amine displacement reaction of a compound of the formula R1R2NHBH2C(O)OH comprises allowing a Lewis base adduct of BH2CO2H, such as a primary, secondary or tertiary amine, a heterocyclic amine, an aryl phosphine, capable of being displaced by the displacing Lewis base at a temperature of 20 to 20 C. The preferred Lewis base adduct compounds of BH2CO2H contemplated within the scope of the present invention are tri-lower alkyl amines wherein each alkyl group contains 1 to 7 carbon atoms such as trimethyl amine, triethyl amine, and tri-n-propyl amine.

Descriptors :   *PATENT APPLICATIONS, *AMINES, *CHEMOTHERAPEUTIC AGENTS, *CARBOXYL GROUPS, *BORANES, ALKYL RADICALS, ARYL RADICALS, CHOLESTEROL, DISPLACEMENT REACTIONS, HETEROCYCLIC COMPOUNDS, HYDROGEN, METHYL RADICALS, PHOSPHINE, TRIETHYLALUMINUM, LIPIDS

Subject Categories : Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE