So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Yamagishi, Hiroaki; Inoue, Takayuki; Nakajima, Yutaka; Maeda, Jun; Tominaga, Hiroaki; Usuda, Hiroyuki; Hondo, Takeshi; Moritomo, Ayako; Nakamori, Fumihiro; Ito, Misato; Nakamura, Koji; Morio, Hiroki; Higashi, Yasuyuki; Inami, Masamichi; Shirakami, Shohei researched the compound: 2-Cyano-2-methylpropanoic acid( cas:22426-30-8 ).Electric Literature of C5H7NO2.They published the article 《Discovery of tricyclic dipyrrolopyridine derivatives as novel JAK inhibitors》 about this compound( cas:22426-30-8 ) in Bioorganic & Medicinal Chemistry. Keywords: tricyclic dipyrrolopyridine derivative preparation JAK inhibitor immunomodulator transplant bioavailability; Autoimmune diseases; IL-2; Immunomodulator; Janus kinase inhibitor; Organ transplant rejection. We’ll tell you more about this compound (cas:22426-30-8).
Janus kinases (JAKs) play a crucial role in cytokine mediated signal transduction. JAK inhibitors have emerged as effective immunomodulative agents for the prevention of transplant rejection. The authors previously reported that the tricyclic imidazo-pyrrolopyridinone 2 (I) is a potent JAK inhibitor; however, it had poor oral absorption due to low membrane permeability. Here, the authors report the structural modification of compound 2 into the tricyclic dipyrrolopyridine 18a (3-[(3R,4R)-3-(dipyrrolo[2,3-b:2′,3′-d]pyridin-1(6H)-yl)-4-methyl- piperidin-1-yl]-3-oxopropanenitrile ) focusing on reduction of polar surface area (PSA), which exhibits potent in vitro activity, improved membrane permeability and good oral bioavailability. Compound 18a showed efficacy in rat heterotopic cardiac transplants model.
Compounds in my other articles are similar to this one(2-Cyano-2-methylpropanoic acid)Electric Literature of C5H7NO2, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.
Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method