CFI-402257

New Drug Approvals

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CFI-402257

N-cyclopropyl-4-(7-((((1s,3s)-3-hydroxy-3-methylcyclobutyl)methyl)amino)-5-(pyridin-2-yloxy)pyrazolo[1,5-a]pyridin-3-yl)-2-methylbenzamide

N-cyclopropyl-4-(7-( (((Is, 3s)-3-hydroxy-3-methylcyclobutyl)methyl)amino)-5- (pyridin-3-yloxy)pyrazolol 1 , 5-a ]pyrimidin-3-yl)-2-methylbenzamide

CAS 1610759-22-2 (free base); 1610677-37-6 (HCl)
MF: C29H31N5O3
MW: 497.2427

University Health Network

CFI-402257 is a highly potent and selective TTK (threonine tyrosine kinase) Inhibitor ((TTK Ki = 0.1 nM) with potential anticancer activity. TTK is an essential chromosomal regulator and is overexpressed in aneuploid tumors. High TTK levels correlate with a high tumor grade11 and poor patient outcomes. TTK inhibition are associated with a disabled mitotic checkpoint, resulting in chromosome segregation errors, aneuploidy, and cell death.

Synthesis

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SYNTHESIS COLOUR INDICATED

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IF YOU HAVE ENJOYED IT ………EMAIL ME amcrasto@gmail.com, +919323115463, India

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DR ANTHONY CRASTO , WORLDDRUGTRACKER, HELPING MILLIONS, MAKING INDIA AND INDIANS PROUD

Protein kinases have been the subject of extensive study in the search for new therapeutic agents in various diseases, for example, cancer. Protein kinases are known to mediate…

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Quisapride Hydrochloride

New Drug Approvals

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Quisapride Hydrochloride

(R) – quinuclidine-3-5 – ((S) -2 – (( 4 – amino-5-chloro-2-ethoxy benzoylamino) methyl) morpholino) hexanoate

IND Filed china

A 5-HT4 agonist potentially for the treatment of gastrointestinal motility disorders.

SHR-116 958, SHR 116958

CAS 1132682-83-7 (Free)

Shanghai Hengrui Pharmaceutical Co., Ltd.

CAS 1274633-87-2 (dihcl)

  • (3R)-1-Azabicyclo[2.2.2]oct-3-yl (2S)-2-[[(4-amino-5-chloro-2-ethoxybenzoyl)amino]methyl]-4-morpholinehexanoate hydrochloride (1:2)
  • SHR 116958
  • C27 H41 Cl N4 O5 . 2 Cl H,
    4-Morpholinehexanoic acid, 2-[[(4-amino-5-chloro-2-ethoxybenzoyl)amino]methyl]-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, hydrochloride (1:2), (2S)-

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5-HT is a neurotransmitter Chong, widely distributed in the central nervous system and peripheral tissues, 5-HT receptor subtypes at least seven, and a wide variety of physiological functions of 5-HT receptor with different interactions related. Thus, the 5-HT receptor subtypes research is very necessary.

The study found that the HT-5 4 receptor agonists useful for treating a variety of diseases, such as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional…

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PDE4 inhibitor , Sumitomo Dainippon Pharma Company

New Drug Approvals

Figure

2-[2-Methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-benzimidazol-5-yl]-1,3-benzoxazole Hemifumarate

Sumitomo Dainippon Pharma Company,

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CAS FREE FORM 1256966-65-0

Benzoxazole, 2-[2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-benzimidazol-5-yl]-

MF C20 H19 N3 O2, MW, 333.38 FREE FORM
NMR FOR HEMIFUMARATE

1H NMR (400 MHz, DMSO-d6)

δ 13.1 (br, 1H), 8.33 (d, J = 1.5 HZ, 1H), 8.06 (dd, J = 5.1, 1.6 Hz, 1H), 7.89 (d, J = 0.8 Hz, 1H), 7.82–7.76 (m, 2H), 7.43–7.38 (m, 2H), 6.64 (s, 1H), 4.71–4.62 (m, 1H), 4.06 (dd, J = 11.4, 4.3 Hz, 2H), 3.58 (dd, J = 11.7, 11.4 Hz, 2H), 2.67 (s, 3H), 2.47–2.36 (m, 2H), 1.90–1.86 (m, 2H).

13C NMR (100 MHz, DMSO-d6)

δ 165.92, 163.26, 153.94, 150.20, 142.94, 141.75, 136.21, 133.93, 124.94, 124.67, 120.89, 119.40, 117.70, 112.44, 110.72, 66.50, 52.67, 30.70, 14.62.
Compound 1 is a PDE4 inhibitor and is expected to improve memory impairment. In addition to the…

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Copper catalysed alkynylation of tertiary amines with CaC2 via sp3 C-H activation

 

Green Chem., 2016, Advance Article
DOI: 10.1039/C6GC00872K, Communication
Siew Ping Teong, Dingyi Yu, Yin Ngai Sum, Yugen Zhang
A mild and easy-to-handle protocol to produce propargylamines with a terminal alkyne through sp3 C-H bond activation and C-C coupling of tertiary amines and calcium carbide has been developed.

 

Copper catalysed alkynylation of tertiary amines with CaC2 via sp3 C–H activation

*Corresponding authors
aInstitute of Bioengineering and Nanotechnology, 31 Biopolis Way, The Nanos, Singapore 138669, Singapore
E-mail: ygzhang@ibn.a-star.edu.sg
Green Chem., 2016, Advance Article

DOI: 10.1039/C6GC00872K

A mild and easy-to-handle protocol to produce propargylamines with a terminal alkyne through catalytic cross-coupling of tertiary amines and calcium carbide has been developed. The reaction proceeds via sp3 C–H bond activation and C–C coupling. Good to excellent yields were obtained for the corresponding propargylamines with both alkyl and aryl substitutions. The development of these functionalized propargylamines with a terminal alkyne group will offer a wider application for the synthesis of natural or pharmaceutical products due to their unique sp C–H reactivity.
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N-methyl-N-(prop-2-yn-1-yl)cyclohexanamine (3a) This compound was prepared according to general procedure and isolated by column chromatography (ethyl acetate/hexane = 1/8) to give the product as a light yellow liquid (139 mg, 92%). 1H NMR (400 MHz, CDCl3) δ 3.42 (d, J = 2.4 Hz, 2H, CH2), 2.39 – 2.31 (m, 1H, CH), 2.35 (s, 3H, CH3), 2.19 (t, J = 2.5 Hz, 1H, C≡CH), 1.92 – 1.90 (m, 2H, CH2), 1.78 – 1.75 (m, 2H, CH2), 1.62 – 1.59 (m, 1H, CH2), 1.31 – 1.08 (m, 5H, CH2); 13C NMR (101 MHz, CDCl3) δ 79.8, 72.6, 60.7, 42.9, 38.5, 29.8, 26.0, 25.5; HRMS (EI) m/z calcd. for C 10 H 17 N 151.1361; found 151.1358
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/////Copper catalysed alkynylation,  tertiary amines,  CaC2,  sp3 C-H activation

Plastically deformed Cu-based alloys as high-performance catalysts for the reduction of 4-nitrophenol

Catal. Sci. Technol., 2016, Advance Article
DOI: 10.1039/C6CY00734A, Paper
Eredzhep Menumerov, Kyle D. Gilroy, Maryam Hajfathalian, Colin J. Murphy, Erica R. McKenzie, Robert A. Hughes, Svetlana Neretina
Plastically deformed mesoscopic structures exposed to an etching procedure are demonstrated as highly catalytic in the reduction of 4-nitrophenol.

Plastically deformed Cu-based alloys as high-performance catalysts for the reduction of 4-nitrophenol

Plastically deformed Cu-based alloys as high-performance catalysts for the reduction of 4-nitrophenol

The severe plastic deformation of metals leads to the formation of nanotextured surfaces as well as the retention of significant strain energy, characteristics which are known to promote catalytic activity. Here, we demonstrate plastically deformed surfaces of copper and copper-based alloys as being highly catalytic using the well-studied model catalytic reaction which reduces 4-nitrophenol to 4-aminophenol by borohydride. Among the materials studied, the most catalytically active is formed in a two-step process where metal chips are mechanically sheared from a Cu–Sn alloy containing precipitates and then exposed to an etchant which removes the precipitates from the exposed surface. The so-formed structures exhibit exceedingly high catalytic activity and set new benchmarks when incorporated into a fixed-bed reactor. The formation of catalytically active sites is shown to be strongly dependent on the presence of the precipitates during the deformation process, achieving an order of magnitude increase in the reaction rate constant when compared to similarly formed Cu–Sn catalysts lacking these precipitates. The work, therefore, demonstrates a new approach for generating catalytically active sites which may be applicable to other alloy combinations.

 

////Plastically deformed, Cu-based alloys,  high-performance catalysts,  reduction, 4-nitrophenol

Synthesis in mesoreactors: Ru(porphyrin)CO-catalyzed aziridination of olefins under continuous flow conditions

Catal. Sci. Technol., 2016, Advance Article
DOI: 10.1039/C6CY00207B, Communication
S. Rossi, A. Puglisi, M. Benaglia, D. M. Carminati, D. Intrieri, E. Gallo
The Ru(porphyrin)CO-catalyzed addition of aryl azides to styrenes to afford N-aryl aziridines was successfully performed for the first time in mesoreactors under continuous flow conditions.

Synthesis in mesoreactors: Ru(porphyrin)CO-catalyzed aziridination of olefins under continuous flow conditions

S. Rossi,a   A. Puglisi,*a   M. Benaglia,*a   D. M. Carminati,a  D. Intrieria and   E. Galloa  
*Corresponding authors
aDipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, Milano, Italy
E-mail: alessandra.puglisi@unimi.it, maurizio.benaglia@unimi.it
Catal. Sci. Technol., 2016, Advance Article

DOI: 10.1039/C6CY00207B

The Ru(porphyrin)CO-catalyzed addition of aryl azides to styrenes to afford N-aryl aziridines was successfully performed for the first time in mesoreactors under continuous flow conditions. Mesofluidic technology allowed for a rapid screening of different parameters and a quick identification of the optimized reaction conditions.

 

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/////Synthesis in mesoreactors, Ru(porphyrin)CO-catalyzed,  aziridination of olefins,  continuous flow conditions