1,721,066 research outputs found
Peptide Drug Discovery and Process Development Perspectives
No full textThe peptide market will show incredible performances growing from the actual 30 B by the year 2026. This jump is directly related to the improvement of the drug design and development process achieved during the last 10 years (1). In fact, not long time ago, once the active peptide was identified, the drug, a peptidomimetic molecule, was obtained after an extensive medicinal chemistry program. Nowadays, with a few modifications of the natural sequence, it is possible to generate analogue peptides with a controlled conformation and an improved pharmaceutical profile, like long halflife and oral delivery
Steps toward sustainable peptide synthesis: matching alternative solvents, bases and process features
No full textGreen Chemistry Impact and Evolution in the Pharma Industry
No full textThe impact of green chemistry in the pharmaceutical industry is continuously growing thanks to
the efforts of academic and industrial research groups. The design of industrial processes inspired
by the Twelve Principles of Green Chemistry can be guided by green metrics and nowadays
it is relatively simple to stand on the green side when designing the synthesis of a drug
Copper-Free Heck−Cassar−Sonogashira and Suzuki−Miyaura Reactions of Aryl Chlorides: A Sustainable Approach
Full text linkSustainable and efficient aryl halides with copper free Heck−Cassar−Sonogashira (HCS) and Suzuki−Miyaura
(SM) cross-coupling reactions were described. Independently
from the aryl chloride substituents, the green protocol based on
N-hydroxyethylpyrrolidone (HEP)/water as solvents and sodium
2′-dicyclohexylphosphino-2,6-dimethoxy-1,1′-biphenyl-3-sulfonate
(sSPhos) as ligand afforded the target products with a high
turnover number (TON), high reaction mass efficiency (RME),
and low process mass intensity (PMI). The best results have been
obtained with TMG and Cs2CO3 as the base for the HCS and
Cs2CO3 and K2CO3 for the SM coupling. The PMI and RME
achieved are among the best in the field and allowed us to simplify
purification processes that are critical for industrial applications
Development of a practical and sustainable strategy for the synthesis of ST1535 by an iron-catalyzed Kumada cross-coupling reaction
No full textA simple, convenient, and environmentally friendly route to ST1535 employing an iron-catalyzed cross-coupling reaction and butylmagnesium chloride is described
Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives
No full textHistone deacetylase inhibitors (HDACis) are one of the last frontiers in pharmaceutical research. Several classes of HDACi have been identified. Although more than 20 HDACi are under preclinical and clinical investigation as single agents and in combination therapies against different cancers, just two of them were approved by the US FDA: Zolinza® and Istodax®, both licensed for the treatment of cutaneous T-cell lymphoma, the latter also of peripheral T-cell lymphoma. Since HDAC enzymes act by forming multiprotein complexes (clusters), containing cofactors, the main problem in designing new HDACi is that the inhibition activity evaluated on isolated enzyme isoforms does not match the in vivo outcomes. In the coming years, the research will be oriented toward a better understanding of the functioning of these protein complexes as well as the development of new screening assays, with the final goal to obtain new drug candidates for the treatment of cancer
CRYSTALLINE (6R,7R)-7-{2-(5-AMIN0-[1 ,2,4] THIADIAZOL-3-YL)-2-[(Z) TRITYLOXYIMINO]-ACETYLAMINO }-3- [(R)-l'-TERT-BUTOXYCARBONYL-2-0XO [1,3']BIPYRROLIDINYL-(3E) YLIDENEMETHYL ]-8-0X0-5-THIA-1 -AZA BICYCL0[4.2.0]0CT-2-ENE-2-CARBOXYLIC ACID BENZHYDRYL ESTER; ITS MANUFACTURE AND USE
No full textA solid DMSO salvate of a compound of fornula (I) is described, which is a useful intemediate far preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril
Process for the preparation of alectinib
No full textThe present invention relates to a process for preparing alectinib or a pharmaceutically acceptable salt thereof. The present invention also relates to 5 intermediate compounds which are useful in such process and to the preparation of such intermediate compounds. Alectinib is approved as the hydrochloride salt, which is the active ingredient of drug Alecensa® and is intended for oral administration in the form of capsule. It is an anaplastic lymphoma kinase (ALK) inhibitor indicated for the treatment of patients with non-small-cell lung cancer (NSCLC)
PROCESS FOR THE PREPARATION OF PROPOFOL
No full textThe present provides a simple, convenient and time-efficient process for the preparation of propofol. Particularly, the present invention provides an improved process for the preparation of propofol using a heterocyclic base for the decarboxylation reaction. The present invention provides a time-efficient process for the preparation of propofol with high yield and purity
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