Use of High-Throughput Tools for Telescoped Continuous Flow Synthesis of an Alkynylnaphthyridine Anticancer Agent, HSN608 was written by Biyani, Shruti A.;Qi, Qingqing;Wu, Jingze;Moriuchi, Yuta;Larocque, Elizabeth A.;Sintim, Herman O.;Thompson, David H.. And the article was included in Organic Process Research & Development in 2020.Safety of 5-Bromoisoquinolin-8-amine This article mentions the following:
Developing continuous syntheses of lead compounds to support in vivo studies and preclin. evaluation remains an underdeveloped area. We report a telescoped continuous flow synthesis of an alkynylnaphthyridine lead compound for the treatment of FLT3 mutations in acute myeloid leukemia. Different strategies were used to develop the route, including Design of Experiments (DoE), high-throughput experimentation (HTE), and application of desorption electrospray ionization mass spectrometry (DESI-MS) to optimize and telescope the amidation and Sonogashira couplings to prepare the target compound, HSN608 (I), a potent FLT3 inhibitor. Findings from these statistical design and automation studies helped streamline our workflow to achieve 10-fold and 5-fold reductions in the catalyst and cocatalyst loadings, resp., in the synthesis. The application of high-throughput tools combined with a telescoped continuous synthesis method enabled an efficient and safe synthesis of this lead compound using the hazardous coupling reagent HATU while minimizing byproduct formation. In the experiment, the researchers used many compounds, for example, 5-Bromoisoquinolin-8-amine (cas: 90721-35-0Safety of 5-Bromoisoquinolin-8-amine).
5-Bromoisoquinolin-8-amine (cas: 90721-35-0) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Safety of 5-Bromoisoquinolin-8-amine
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem