title: Solid-phase synthesis of 5-substituted amino pyrazoles.
abstract: An efficient method for the solid-supported synthesis of 5-N-alkylamino and 5-N-arylamino pyrazoles is described. This method is general and mild and utilizes readily accessible resin-immobilized beta-ketoamides 2 as starting materials for the preparation of 1. Resin-immobilized beta-ketoamide, aryl-, or alkylhydazine and Lawesson's reagent are suspended in a mixture of THF/Py and heated at 50-55 degrees C to give a resin-bound 5-aminopyrazole, that is liberated from the solid support by treatment with TFA.
authors: Early Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, New Jersey 08543-4000, USA. dharmpal.dodd@bms.com
authors: Dharmpal S
authors: DS
authors: Dodd
authors: Rogelio L
authors: RL
authors: Martinez
authors: Muthoni
authors: M
authors: Kamau
authors: Zheming
authors: Z
authors: Ruan
authors: Katy
authors: K
authors: Van Kirk
authors: Christopher B
authors: CB
authors: Cooper
authors: Mark A
authors: MA
authors: Hermsmeier
authors: Sarah C
authors: SC
authors: Traeger
authors: Michael A
authors: MA
authors: Poss
mesh_terms: D000588:Amines / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry*
chemical_list: D000588:Amines; D011720:Pyrazoles