Biological functions of small molecules are often closely related to their stereochemistry. Stereoisomers of the same scaffolds can sometimes show complementary biological responses, as exemplified by the cis- and trans-4,5-diaryl-2-imidazolines. Chapter I summarizes the recent progress of researches on application and synthesis of 2-imidazolines. Chapter II describes an efficient synthetic methodology of converting trans-4,5-diaryl-2-imidazolines to the corresponding cis-4,5-diaryl-2-imidazolines. This methodology features mild reaction conditions and a simple one-pot two-step procedure.
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