On November 30, 2021, Zhang, Weidong; Sun, Qingyan; Zhao, Menghao; Chen, Haomin; Guo, Jingwen; Zhang, Panpan published a patent.Name: 1-Bromo-3-isocyanato-2-methyl-benzene The title of the patent was Preparation of cyclopentene compounds as STAT3 inhibitor for prevention and/or treatment of cell proliferative diseases. And the patent contained the following:
The present invention relates to the preparation of cyclopentene compounds as STAT3 inhibitor for prevention and/or treatment of cell proliferative diseases. In particular, the cyclopentene compound I (wherein, ring A = C6-C10 aryl group or 5-6 membered heteroaryl group and the heteroatom in the 5-6 membered heteroaryl group = one or more of N, O, S and the number of heteroatoms = 1-4; n = 0,1,2,3 or 4; R2 = independently C1-C6 alkyl group, C1-C6 alkyl group -O-, C1-C6 alkyl group -C(=O)-N(R2a)- etc.; R2a and R2b = independently H or C1-C4 alkyl group; L1 = -C(=O)-, -N(R11)-C(=O)-N(R10)-, -C(=O)-N(R12)-, -N(R13)-C(=O)- etc., where R10, R11, R12, R13, R14, R15, R16, R17, R18, R19 and R20 = independently H or C1-C4 alkyl group). Further, (R1 = H, C1-C6 alkyl substituted with one or more substituents Ra, C3-C10 cycloalkyl group, C3-C10 cycloalkyl substituted by one or more substituents Rb, C6-C10 aryl group, C3-C10 aryl substituted by one or more substituents Rc, 5-10 membered heterocycloalkyl etc., and the heteroatom = N, O, S etc., and the number of heteroatoms = 1-3; Ra, Rb, Rc, Rd, Re = independently (R1a R1b) N-C(=O)-, C1-C6 alkyl -O-, C1-C6 alkyl -C(=O)-N(R1c)- or O=). Further, (R1a, R1b and R1c = independently H or C1-C4 alkyl group; alternatively, R2 is connected to C or N in R1-L1 to form a 4-7 membered heterocycloalkyl group together with the atoms connected to ring A; the heteroatoms in the 4-7 membered heterocycloalkyl group = one or more of N, O, S, S(=O) and S(=O)2, and the number of heteroatoms = 1-3; the 4-7 membered heterocycloalkyl group is optionally substituted by the substituents: C1-C4 alkyl group or =O; a carbon atom with * represents a chiral carbon atom, which is in the S configuration, R configuration, or a mixture) or its pharmaceutically acceptable salt was prepared The inventive cyclopentene compounds has selectivity for STAT3 in preliminary activity study, and at the same time, shows a strong inhibitory activity against tumor cell proliferation with a significant killing effect on human cancer cells, especially human breast cancer cell line MDA-MB-231, human prostate cancer cell line PC-3 and human prostate cancer cell line DU-145, therefore it can be used as a series of novel STAT3 inhibitors in the preparation of corresponding novel antitumor drugs for diseases with a good market prospect. The experimental process involved the reaction of 1-Bromo-3-isocyanato-2-methyl-benzene(cas: 1261475-16-4).Name: 1-Bromo-3-isocyanato-2-methyl-benzene
The Article related to cyclopentene compound stat3 inhibitor antitumor agent, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Name: 1-Bromo-3-isocyanato-2-methyl-benzene
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary