Mega Innovative Crops Pvt. Ltd., GIDC Estate Panoli, Ankleshwar-394 116, Gujarat, India Department of Chemistry, SGB Amravati University, Amravati-444 602, Maharashtra, India E-mail: mtshaikh31@gmail.com, aswaranand@gmail.com Manuscript received online 30 December 2019, revised 24 February 2020, accepted 26 February 2020 Environmental pollution generated due to industrial and other sources is big issue in our regular discussion; in order to prevent the pollution here we have initiated work involving green chemistry principles. Here, we have developed a process as ���Green novel one pot synthesis of dexethylphenidate hydrochloride with significantly high yield and purity���. In the present work a special attention has been focus on the available regulations, the toxicological background for establishing limits, as well as the organic synthetic research with an analytical approach towards chiral assessment. This paper provides a complete overview of the topic with current available information, to address the overall chiral as well as hazardous issue during the development of new drug substances in R & D for the benefits to society.