Sequential C-Selective Difluoromethylation/Pd-Catalyzed Decarboxylative Protonation: An Efficient Access to Tertiary Difluoromethylated Scaffolds

2019 ◽  
Author(s):  
Nicolas Duchemin ◽  
Roberto Buccafusca ◽  
Marc Daumas ◽  
Vincent Ferey ◽  
Stellios Arseniyadis
Keyword(s):  
Drug Development ◽  
Late Stage ◽  
Efficient Access ◽  
Palladium Catalyzed ◽  
General Method

We report here a general method that allows a highly straightforward access to tertiary difluoromethylated compounds. The strategy relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and an unprecedented palladium-catalyzed decarboxylative protonation. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.<br>

Sequential C-Selective Difluoromethylation/Pd-Catalyzed Decarboxylative Protonation: An Efficient Access to Tertiary Difluoromethylated Scaffolds

2019 ◽  
Author(s):  
Nicolas Duchemin ◽  
Roberto Buccafusca ◽  
Marc Daumas ◽  
Vincent Ferey ◽  
Stellios Arseniyadis
Keyword(s):  
Drug Development ◽  
Late Stage ◽  
Efficient Access ◽  
Palladium Catalyzed ◽  
General Method

We report here a general method that allows a highly straightforward access to tertiary difluoromethylated compounds. The strategy relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and an unprecedented palladium-catalyzed decarboxylative protonation. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.<br>

Reductive Cleavage of Secondary Sulfonamides: Converting Terminal Functional Groups into Versatile Synthetic Handles

2019 ◽  
Author(s):  
Patrick Fier ◽  
Suhong Kim ◽  
Kevin M. Maloney
Keyword(s):  
Functional Groups ◽  
Late Stage ◽  
Reductive Cleavage ◽  
Bioactive Molecules ◽  
General Method

Sulfonamides are pervasive in drugs and agrochemicals, yet are typically considered as terminal functional groups rather than synthetic handles. To enable the general late-stage functionalization of secondary sulfonamides, we have developed a mild and general method to reductively cleave the N-S bonds of sulfonamides to generate sulfinates and amines, components which can further react <i>in-situ</i> to access a variety of other medicinally relevant functional groups. The utility of this platform is highlighted by the selective manipulation of several complex bioactive molecules.

scholarly journals Precision Medicine: From “Omics” to Economics towards Data-Driven Healthcare - Time for European Transformation

2017 ◽  
Vol 2 (Suppl. 1) ◽  
pp. 1-10 ◽  
Author(s):  
Denis Lacombe ◽  
Lifang Liu ◽  
Françoise Meunier ◽  
Vassilis Golfinopoulos
Keyword(s):  
Drug Development ◽  
Development Process ◽  
Precision Oncology ◽  
Drug Development Process ◽  
Cancer Treatments ◽  
True Value ◽  
Efficient Access ◽  
Funding Agencies ◽  
Anti Cancer

There is room for improvement for optimally bringing the latest science to the patient while taking into account patient priorities such as quality of life. Too often, regulatory agencies, governments, and funding agencies do not stimulate the integration of research into care and vice versa. Re-engineering the drug development process is a priority, and healthcare systems are long due for transformation. On one hand, patients need efficient access to treatments, but despite precision oncology approaches, efficiently shared screening platforms for sorting patients based on the biology of their tumour for trial access are lacking and, on the other hand, the true value of cancer care is poorly addressed as central questions such as dose, scheduling, duration, and combination are not or sub-optimally addressed by registration trials. Solid evidence on those parameters could potentially lead to a rational and wiser use of anti-cancer treatments. Together, optimally targeting patient population and robust comparative effectiveness data could lead to more affordable and economically sound approaches. The drug development process and healthcare models need to be interconnected through redesigned systems taking into account the full math from drug development into affordable care.

scholarly journals Palladium-Catalyzed Late-Stage Direct Arene Cyanation

Chem ◽  
2019 ◽  
Vol 5 (1) ◽  
pp. 97-107 ◽  
Author(s):  
Da Zhao ◽  
Peng Xu ◽  
Tobias Ritter
Keyword(s):  
Late Stage ◽  
Palladium Catalyzed

Palladium-catalyzed C(sp2)–H aminoimidoylation of isocyano-containing arenes: synthesis of amino substituted N-heterocycles

2017 ◽  
Vol 4 (9) ◽  
pp. 1768-1771 ◽  
Author(s):  
Zhuang Xiong ◽  
Jian Wang ◽  
Yanbo Wang ◽  
Shuang Luo ◽  
Qiang Zhu
Keyword(s):  
Efficient Access ◽  
Palladium Catalyzed ◽  
Isoquinoline Derivatives

An efficient access to amino substituted phenanthridine and isoquinoline derivatives, through palladium-catalyzed C(sp2)–H aminoimidoylation, has been developed.

Palladium-Catalyzed Regioselective Direct C-H Bond Alkoxycarbonylation of 2-Arylimidazo[1,2-a]pyridines

2021 ◽  
Author(s):  
Ebrahim Kianmehr ◽  
Arezoo Tanbakouchian
Keyword(s):  
Efficient Access ◽  
Palladium Catalyzed

A palladium-catalyzed practical and efficient access to alkoxycarbonylated imidazo[1,2-a]pyridines at C-3 position has been developed relaying on the association of W(CO)6 as a safe and easy to handle CO surrogate...

Secondary Phosphine Oxide Preligands for Palladium-Catalyzed C-H (Hetero)Arylations: Efficient Access to Pybox Ligands

2017 ◽  
Vol 359 (18) ◽  
pp. 3137-3141 ◽  
Author(s):  
Debasish Ghorai ◽  
Valentin Müller ◽  
Helena Keil ◽  
Dietmar Stalke ◽  
Giuseppe Zanoni ◽  
...  
Keyword(s):  
Phosphine Oxide ◽  
Secondary Phosphine ◽  
Efficient Access ◽  
Palladium Catalyzed
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