40675-45-4Relevant articles and documents
Direct Transformation of Arylamines to Aryl Halides via Sodium Nitrite and N-Halosuccinimide
Mukhopadhyay, Sushobhan,Batra, Sanjay
supporting information, p. 14622 - 14626 (2018/09/21)
A one-pot universal approach for transforming arylamines to aryl halides via reaction with sodium nitrite (NaNO2) and N-halosuccinimide (NXS) in DMF at room temperature under metal- and acid-free condition is described. This new protocol that is complementary to the Sandmeyer reaction, is suggested to involve the in situ generation of nitryl halide induce nitrosylation of aryl amine to form the diazo intermediate which is halogenated to furnish the aryl halide.
Deuterium-modified Abemaciclib derivative
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Paragraph 0138; 0139; 0140; 0141; 0142, (2017/08/02)
The invention belongs to the field of medicinal chemistry and specifically relates to a deuterium-modified Abemaciclib derivative, a preparation method of the derivative, a pharmaceutical composition containing the deuterium-modified Abemaciclib derivative, and application of the deuterium-modified Abemaciclib derivative and the pharmaceutical composition in the preparation of a medicine for treating cell proliferative diseases. In comparison with Abemaciclib, some compounds of the invention (especially compounds in the embodiment) have more excellent pharmacokinetic properties. It is expected that clinical dosage will be reduced. Thus, treatment cost is reduced so as to benefit more patients.
An efficient synthesis of radiolabelled SANT-1
Zhang, Yinsheng,Stolle, Wayne T.
scheme or table, p. 487 - 489 (2011/05/05)
SANT-1, (4-benzyl-N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-1- piperazinamine), is a reference compound and used for establishing a biological assay for the smoothened receptor (SMO). Preparation of radiolabelled material was needed for establishing radioligand protein/receptor binding studies. [ 3H]SANT-1 was prepared with a radiochemical purity of >95% (25 Ci/mmol) using direct Crabtree catalyzed T/H exchange method, while [ 14C]SANT-1 was synthesized at 98.2% radiochemical purity (54 mCi/mmol) using [14C]dimethylformamide. The details of the syntheses of radioactive labelled SANT-1 were presented. Copyright