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A borrowing hydrogen methodology: palladium-catalyzed dehydrative...
A borrowing hydrogen methodology: palladium-catalyzed dehydrative N-benzylation of 2-aminopyridines in water Hidemasa Hikawa,*a Hirokazu Imamura,a Shoko Kikkawaa and Isao Azumaya*a Author...
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ICH Q12: Guideline on Technical and Regulatory Considerations for...
ICH Q12: Guideline on Technical and Regulatory Considerations for Pharmaceutical Product Lifecycle Management, 1-2 Recent ICH quality guidelines (Q8–Q11)(3−6) have focused on providing guidance on the...
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Elemental Impurities
Elemental Impurities On January 1, 2018, new guidelines regarding elemental impurities in brand and generic drug products went into effect. Elemental impurities, such as arsenic and lead, pose...
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National award to Anthony Melvin Crasto for contribution to Pharma society...
DR ANTHONY MEVIN CRASTO Conferred prestigious individual national award at function for contribution to Pharma society from Times Network, National Awards for Marketing Excellence ( For Excellence...
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EMA modernizing the orphan designation process
EMA modernizing the orphan designation process On June 19, 2018, the European Medicines Agency (EMA) launched a new secure online portal for Orphan Designation (OD) applications. The portal, named...
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Advancing Flow Chemistry Portability: A Simplified Approach to Scaling Up...
We report mixing characterization of five lab-scale and eight production-scale static mixers using a modified fourth Bourne reaction. An efficient inline method relying on UV–vis spectroscopy was...
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Copper-catalyzed pyrrole synthesis from 3,6-dihydro-1,2-oxazines
Copper-catalyzed pyrrole synthesis from 3,6-dihydro-1,2-oxazines Naoki Yasukawa,a Marina Kuwata,a Takuya Imai,a Yasunari Monguchi,a Hironao Sajiki*a and Yoshinari Sawama*a Author affiliations...
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A versatile biosynthetic approach to amide bond formation
A versatile biosynthetic approach to amide bond formation Helena K. Philpott,a Pamela J. Thomas,b David Tew,a Doug E. Fuerstc and Sarah L. Lovelock*a Author affiliations *Corresponding authors...
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Anthony Melvin Crasto gets International award for Outstanding contribution...
Conferred CMO Asia award 2018 singapore Shobha and Aishal crasto collect my International award for Excellence in Pharma by CMO ASIA 31st July 2018 | at an award function in Le Méridien Singapore,...
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Development and Scale-Up of a Continuous Reaction for Production of an Active...
Flow reactor equipment that was used in the piloting of the aldol flow chemistry. (a) The tube-in-shell heat exchangers were used to control stream temperature upstream and downstream of the (b)...
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Ethyl 4, 6-dichloro-1H-indole-2-carboxylate
Ethyl 4, 6-dichloro-1H-indole-2-carboxylate ethyl 4,6-dichloro-1H-indole-2-carboxylate (1a) (2.70 kg, 99.5%). Mp 187–188 °C; HRMS (ESI) m/z [M – H]− calcd for C11H8NO2Cl2 255.9927, found 255.9930; 1H...
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Process Development of Febuxostat Using Palladium- and Copper-Catalyzed C–H...
There is significant interest in the development of process routes for active pharmaceutical ingredients using C–H arylation methodology. An efficient and practical synthetic route for febuxostat (1),...
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Crystallization
Crystallization is the (natural or artificial) process by which a solid forms, where the atoms or molecules are highly organized into a structure known as a crystal. Some of the ways by which crystals...
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1-(4-Cyanophenyl)piperazine
1-(4-Cyanophenyl)piperazine 1-(4-Cyanophenyl)piperazine (1a).1 Isolated as a mixture of mono (1a) and di (3) arylated products ~9:1. Conversion: quantitative. Peaks attributed to 1a: 1H NMR (400 MHz,...
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Development of an SNAr Reaction: A Practical and Scalable Strategy To...
A simple and operationally practical method to sequester and remove fluoride generated through the SNAr reaction between amines and aryl fluorides is reported. Calcium propionate acts as an...
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A call to (green) arms: a rallying cry for green chemistry and engineering...
A call to (green) arms: a rallying cry for green chemistry and engineering for CO2 capture, utilisation and storage Julien Leclaire*a and David J. Heldebrant*b Author affiliations *Corresponding...
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3-fluoro-4- morpholinoaniline
3-fluoro-4- morpholinoaniline 1H NMR (400MHz, CDCl3) 6.82 (m, 1H, ArH), 6.43 (m, 2H, 2xArH), 3.87 (m, 4H, 2xCH2O), 3.58 (brs, 2H, NH2), 2.99 (m, 4H, 2xCH2N). 13C NMR (100MHz, CDCl3) 156.9 (d J=...
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4-(2-fluoro-4-nitrophenyl)morpholine
4-(2-fluoro-4-nitrophenyl)morpholine 1H NMR (400MHz, CDCl3) 8.03 (ddd J=1.0, 2.6 and 9.0Hz, 1H, ArH), 7.94 (dd J=2.6 and 13.1Hz, 1H, ArH), 6.94 (t J=8.7Hz, 1H, ArH), 3.90 (t J=4.7Hz, 4H, 2xCH2O),...
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2-amino-4-bromo-5-fluorobenzoic acid
2-amino-4-bromo-5-fluorobenzoic acid as a white to off-white crystalline solid 1H NMR (400 MHz, DMSO-d6) δ 7.62 (d, J=9.6 Hz, 1H), 7.21-6.5 (m, 3H), 3.8- 3.3 (br s, 1H). 13C NMR (100 MHz, DMSO-d6)...
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Quetiapine
Quetiapine 1H NMR (400 MHz, CD3OD): δ = 3.18-3.27 (m, 4H), 3.35-3.44 (m, 3H), 3.56-3.58 (m, 3H), 3.67-3.69 (m, 3H), 3.76 (t, J = 5.2 Hz, 2H), 4.32 (s, 1H), 6.88 (td, J = 7.4 Hz, 1.2 Hz, 1H), 7.04 (dd,...
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