Among various participations in the global efforts for drugs, preservatives and pesticides discovery, there are cost-effective simple synthetic routes via productive methods to synthesize potent biologically active compounds, utilizing biomass driven starting compounds. This eco-friendly approach appropriates also researchers where shortage in research fund and facilities. Versatile precursors such as 3-oxoalkane carboxylates ,activated nitriles and ,β unsaturated ketones, were utilized for the facile synthesis of various biologically interesting small molecules. In this review, we highlight representative synthetic findings for bioactive leads arising from our continuous attempts with this approach. Further development by industry and academia through lead optimization will produce new active ingredients to face contiguous hazard biological challenges and resistance of microbes and insects. Many other researchers have made many great achievements in each of these subjects, but these are beyond the scope of this review.