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.
Deuterated diphenylaminopyrimidine compound
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Paragraph 0144; 0145; 0146; 0147, (2017/05/10)
The invention belongs to the field of medicine, and relates to a deuterated diphenylaminopyrimidine compound or a pharmaceutically acceptable salt thereof, and more particularly to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition thereof and application thereof in the treatment of a cell proliferative disease.
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.
HYDRAZIDE CONTAINING NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
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Page/Page column 73, (2013/03/26)
The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
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
Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate Gi proteins
Manetti, Dina,Mannelli, Lorenzo Di Cesare,Dei, Silvia,Galeotti, Nicoletta,Ghelardini, Carla,Romanelli, Maria Novella,Scapecchi, Serena,Teodori, Elisabetta,Pacini, Alessandra,Bartolini, Alessandro,Gualtieri, Fulvio
, p. 6491 - 6503 (2007/10/03)
Heterotrimeric G proteins play a pivotal role in the communication of cells with the environment. G proteins are stimulated by cell surface receptors (GPCR) that catalyze the exchange of GDP, bound to Gα subunit, with GTP and can per se be the target of drugs. Based on the structure of two nonpeptidic modulators of Gi proteins, a series of new molecules characterized by a long hydrophobic chain and at least two nitrogen atoms protonated at physiological pH was designed. The compounds were tested for their ability to stimulate binding of GTPγS to recombinant Gi proteins. Gi activation properties were also evaluated by inhibition of adenylyl cyclase activity in intact lymphocytes. Most compounds were able to stimulate GTPγS binding and to inhibit cAMP production at micromolar doses. Among the active compounds, 34 showed good efficacy and was the most potent compound studied, particularly on αo subtype; its regioisomer, 36, was the most efficacious one. Compound 7 showed also an interesting profile as it showed selectivity toward the αo subtype, in both efficacy and potency. Some of the compounds synthesized and found to be active may be useful leads to develop more potent and selective Gi protein modulators.
Biologically active compounds
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, (2008/06/13)
Biologically active geldanamycin derivatives of Formula III, SPC1 wherein R5, R6, R7 and R8 are the same or different and selected from hydrogen, hydroxy, halo, alkyl, alkoxy, carboxyl, carboalkoxyl, amino, amido, or N-alkylsubstituted amido; pharmaceutical compositions and therapeutic methods involving the same.
