Pharmacological Active Amine-Carboxyboranes.
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.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 17, 1986
- Accession Number
- ADD012607
Entities
People
- Andrew T. McPhail
- Bernard G. Spielvogel
- Iris H. Hall
Organizations
- United States Army