On March 17, 2022, Ryu, Hyung-Chul; Kim, Jae-Sun; Lim, Jee-Woong; Lee, Ju Young; Choi, Kwanghyun; Rajesh, Rengasamy; Chang, Duk-Ho; Gwon, Hyeok Jun; Kang, Hyo Jin published a patent.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of pyrimidinamine derivatives for suppressing EGFR mutant cancer and pharmaceutical use thereof. And the patent contained the following:
The invention relates to pyrimidinamine derivatives of formula I, pharmaceutically acceptable salts, or pharmaceutical compositions thereof which have the activity of inhibiting and/or degrading mutant EGFR protein and are useful for the treatment or prevention of cancer with EGFR mutation, especially lung cancer. The present disclosure also provides a method for the treatment or prevention of EGFR mutation cancer, especially lung cancer, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing same to a subject in need of treatment. Compounds of formula I wherein R1 and R2 are independently H, (halo)alkyl, or trideuteromethyl; R3 – R6 are independently H, halo, cyano, (halo)alkyl, (halo)alkoxy, etc.; m and n are independently 0-4; A is heterocyclyl; L is a connecting group through covalent bond; B is Q1 or Q2; X is single bond, (CH2)1-6, O-(CH2)0-6, C(O)-(CH2)0-6, N(R13)-(CH2)0-6, C(O)-N(R13)-(CH2)0-6, N(R13)-C(O)-(CH2)0-6, etc.; W is C(R14)2 or C(O); R8 is H, hydroxy, halo, (halo)alkyl, or (halo)alkoxy; R9 and R10 are independently H or alkyl; R13 and R14 are independently H or alkyl; o and p are independently 1-3; Y is (halo)alkyl, aryl, etc.; Z is O or S; R11 is H, alkyl, or (CH2)1-6-C(O); R12 is H, alkyl, or cycloalkyl; are claimed. The invention compounds were evaluated for the EGFR protein degradation activity (biol. data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate
The Article related to pyrimidinamine derivative preparation egfr mutant lung cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics