Brief introduction of Safety of trans-3-Aminocyclobutanol hydrochloride

The synthetic route of 1205037-95-1 has been constantly updated, and we look forward to future research findings.

Adding a certain compound to certain chemical reactions, such as: 1205037-95-1, trans-3-Aminocyclobutanol hydrochloride, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Safety of trans-3-Aminocyclobutanol hydrochloride, blongs to alcohols-buliding-blocks compound. Safety of trans-3-Aminocyclobutanol hydrochloride

General Method C (Amine substitution) A solution of benzoimidazol-2-yl arylpyridinone bistriflate derivate (1 equiv) in MeCN, DCM, or DMF was treated with amine (1.2-3 equiv). In the case where the amine is a salt (e.g. HCl), the amine salt was dissolved in MeOH or DMF and passed through a PoraPak Rxn CX ion exchange column to yield the free base which was added to the reaction mixture. The reaction mixture was stirred at rt or up to 45 C for 1-48 h. Solvent was removed and the crude product was purified by column chromatography or prep-HPLC to give the desired product. General Method D (Global deprotection) A solution of protected benzoimidazol-2-yl arylpyridinone derivate (1 equiv) in TFA/conc. HCl (7: 1 v/v) was heated at 80-100 C for 3-24 h. Solvent was removed and the crude product was purified by column chromatography (free base) or prep-HPLC (TFA salt) to give the desired product. To generate the desired product as a HCl salt, the free base was dissolved in MeOH and 1 M HCl-Et20 (2-4 equiv) was added at rt. The solution was stirred for 5 min and azeotroped twice with MeOH.

The synthetic route of 1205037-95-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; UNIVERSITY HEALTH NETWORK; SAMPSON, Peter Brent; PATEL, Narendra Kumar B.; PAULS, Heinz W.; LI, Sze-Wan; NG, Grace; LAUFER, Radoslaw; LIU, Yong; LANG, Yunhui; (93 pag.)WO2016/205942; (2016); A1;,
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