Abstract
After making a new series of spiro[cycloalkane]pyridazinones with high Fsp3 character available, the new target was to synthesize derivatives comprising nitrogen-containing heterocycles, such as triazolo or tetrazolo rings. The corresponding thioxo derivatives (1a,b) seemed to be good starting materials for the synthesis of tetrazolo derivatives. The reaction of the pyridazinethiones (1a,b) with hydrazine surprisingly resulted in Schiff bases (3a,b) deriving from the reaction of hydrazones (2a,b) with acetone.
Highlights
The molecule bank of a company might play an important role in the early phase of preclinical drug discovery
Lovering introduced the Fsp3 character, which usually shows a good correlation with logP and other physicochemical parameters [9,10]
Synthesis of hydrazone and tetrazolo derivatives startingstarting from spiro[cycloalkane]pyridazinethiones. dazinethiones
Summary
The molecule bank of a company might play an important role in the early phase of preclinical drug discovery. In the design of new compounds for a molecule bank, the application of some widely used rules (Lipinski rule of five, Veber’s rule) [2,3,4] and other concepts of medicinal chemistry, such as the role of aromatic rings or bioisosteric nitrogen-containing heterocycles, are of key importance [5,6,7,8]. With the consideration of the above aspects, a series of spiro[cycloalkane]pyridazinones with high Fsp character and advantageous physicochemical parameters was synthetized [11,12,13]. 1. Synthesis of hydrazone and tetrazolo derivatives from spiro[cycloalkane]pyriScheme. 1. Synthesis of hydrazone and tetrazolo derivatives startingstarting from spiro[cycloalkane]pyridazinethiones
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