- Sequential one-pot access to molecular diversity through aniline aqueous borylation
-
On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.
- Erb, William,Albini, Mathieu,Rouden, Jacques,Blanchet, Jrme
-
p. 10568 - 10580
(2015/01/08)
-
- HYDROXAMIC ACID DERVICATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY
-
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: formula (I) wherein Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR5-, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, AIk1, AIk2 and Q are as defined in the claims; z is O or 1 ; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y); wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroary(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.
- -
-
-