146328-84-9

Upstream product

• 143-66-8 sodium tetraphenyl borate 
• 146328-85-0 5-bromo-2-fluoro-benzoic acid 
• 98-80-6 phenylboronic acid 
• 124-38-9 carbon dioxide 
• 324-74-3 4-fluoro-biphenyl 

Downstream Products

• 1397226-08-2 C₂₁H₁₇FN₂O₂S 

Relevant academic research and scientific papers

ACLY INHIBITORS AND USES THEREOF

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A

A high-throughput screen for inhibitors of the histone acetyltransferase, KAT6A, led to identification of an aryl sulfonohydrazide derivative (CTX-0124143) that inhibited KAT6A with an IC50 of 1.0 μM. Elaboration of the structure-activity relationship and medicinal chemistry optimization led to the discovery of WM-8014 (97), a highly potent inhibitor of KAT6A (IC50 = 0.008 μM). WM-8014 competes with acetyl-CoA (Ac-CoA), and X-ray crystallographic analysis demonstrated binding to the Ac-CoA binding site. Through inhibition of KAT6A activity, WM-8014 induces cellular senescence and represents a unique pharmacological tool.

ARYL SULFONOHYDRAZIDES

Compound of formula (I) wherein A is selected from (i), where RF1 is H or F; (ii); (iii) a N-containing C6 heteroaryl group; and B is (B), where X1 is either CRF2 or N, where RF2 is H or F; X2 is either CR3 or N, where R3 is selected from H, Me, CI, F OMe; X3 is either CH or N; X4 is either CRF3 or N, where RF3 is H or F; where only one or two of X1, X2, X3 and X4 may be N; and R4 is selected from I, optionally substituted phenyl, optionally substituted C5-6 heteroaryl; optionally substituted C1-6 aIkyI and optionally substituted C1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.

EP2 RECEPTOR AGONISTS

A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L′ is a single bond, —O— or —C(═O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.

Palladium charcoal-catalyzed, ligandless Suzuki reaction by using tetraarylborates in water

In water and without using any ligand, palladium charcoal-catalyzed Suzuki coupling reaction of tetraarylborates with aryl bromides could be achieved in excellent yield. A concise mechanism consisting of four catalytic cycles is depicted in this paper.

NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intell

Synthesis of Monomeric and Oligomeric Naphtho- and Biaryl-fused 1,8-Diaza-14-crown-4 Macrocycles

Efficient syntheses of naphtho- and biaryl-fused 1,8-diaza-14-crown-4 macrocycles 4a, 4b, 7a, and 7b and related oligomeric systems 11 and 15 are described.An X-ray structure determination for the N,N-dicyanomethyl substituted macrocycle 8 is reported.

Fluorine as an ortho-directing group in aromatic metalation: Generality of the reaction and the high position of fluorine in the Dir-Met potency scale

Many para-substituted fluorobenzenes can be lithiated ortho to fluorine in moderate to good yields, often with one of the dialkylamide bases, lithium diisopropylamide (LDA) or lithium 2,2,6,6-tetramethylpiperidide (LiTMP). Intramolecular competition experiments reveal that fluorine is one of the most potent Dir-Met activating groups under these conditions.