681439-91-8Relevant academic research and scientific papers
NEW COMPOUNDS INHIBITORS OF THE YAP/TAZ-TEAD INTERACTION AND THEIR USE IN THE TREATMENT OF MALIGNANT MESOTHELIOMA
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Page/Page column 33-34, (2017/05/02)
The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. The compounds of formula (I) are inhibitors of the YAP/TAZ-TEAD intera
Directed Ortho metalation-cross coupling strategies. N-cumyl arylsulfonamides. Facile deprotection and expedient route to 7- and 4,7-substituted saccharins
Blanchet, Jerome,Macklin, Todd,Ang, Patrick,Metallinos, Costa,Snieckus, Victor
, p. 3199 - 3206 (2008/02/04)
(Chemical Equation Presented) By using the powerful N-cumylsulfonamide directed metalation group (DMG), a series of 2-substituted derivatives were prepared according to the directed ortho metalation (DoM) tactic (Table 1). Mild conditions for N-decumylation and other simple transformations of the products have been achieved (Scheme 2). The 3-silyloxy sultam 12 undergoes further DoM to give formyl, thiomethyl, iodo, and amide derivatives 13a-g of potential value for saccharin synthesis (Table 2). An effective route to target 7-aryl saccharins via Suzuki cross coupling (Table 3) followed by further metalation-carbamoylation and cyclization (Table 5) is described. 4,7-Disubstituted saccharins have been obtained by similar sequences (Scheme 3). Mild TFA-mediated N-decumylation furnishes substituted primary arylsulfonamides (Table 4).
ortho-anisylsulfonyl as a protecting group for secondary amines: Mild Ni0-catalyzed hydrodesulfonylation
Milburn, Robert R.,Snieckus, Victor
, p. 892 - 894 (2007/10/03)
A potentially good alternative to the tosyl group (Ts) as a protecting group for amines is N-ortho-anisylsulfonyl (Ans), which is readily cleaved under mild, Ni0-catalyzed reductive conditions (see scheme, acac = acetylacetonate). N-Anisylation of primary amines followed by alkylation and deprotection provides a route to a range of secondary amines.
