Diversification of pharmaceutical molecules via late-stage C(sp^(2))–H functionalization

C–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds’bioactivity.Significant advances in this field have been achieved in the past few years,mainly,the C–H functionalization system in(hetero)aryl C–H activation owing to the importance of(hetero)aryl moiety in pharmaceutical.In this review,we described the selected recent examples of how developed intermolecular C(sp^(2))–H functionalization methodologies involving diverse techniques diversify pharmaceutical molecules in the late stage.

Polymorphism of pharmaceutical molecules:perspectives on nucleation

Polymorphism is a widespread phenomenon observed in more than half of all drug substances.Various polymorphs frequently possess different physical,chemical,mechanical and thermal properties that can profoundly affect the bioavailability,stability and other performance characteristics of the drug.Accordingly,the elucidation of the relationship between the particular polymorph of a pharmaceutical molecule and its functional properties is crucial to select the most suitable polymorph of the pharmaceutical molecule for development into a drug product.This review briefly introduces recent advances in the discovery and control of the polymorphs of pharmaceutical molecules,in terms of the enhancement of the selective nucleation of a particular polymorph.In the light of this,some cases discussed in the following is to be considered controversial.