21192-61-0

Upstream product

• 151-50-8 potassium cyanide 
• 32752-54-8 4-(bromomethyl)benzophenone 
• 143-33-9 sodium cyanide 
• 18293-53-3 2-trimethylsilylacetonitrile 
• 90-90-4 (4-bromophenyl)(phenyl)methanone 
• 7677-24-9 trimethylsilyl cyanide 
• 773837-37-9 sodium cyanide 
• 42728-62-1 4-chloromethylbenzophenone 
• 876-08-4 p-(chloromethyl)benzoyl chloride 
• 98-80-6 phenylboronic acid 
• 1071-36-9 sodium cyanoacetate 
• 134-84-9 4-Methylbenzophenone 

Downstream Products

• 26077-80-5 (4-benzoylphenyl)acetic acid 
• 82820-08-4 C₂₃H₁₆N₄O₂ 
• 412049-86-6 2-(4-benzoylphenyl)-N-prop-2-ynylethanamide 
• 412049-87-7 5-[propargyl{2-(4-benzoylphenyl)acetamido}]-2'-deoxy-5'-O-(4,4'-dimethoxytrityl)-uridine 
• 24021-61-2 2-(4-benzoyl-phenyl)-2-methyl-propionic acid methyl ester 
• 1356067-51-0 (+/-)-oxiran-2-ylmethyl 2-(4-benzylphenyl)acetate 
• 1356067-55-4 (±)-tetrahydro-2H-pyran-2-ylmethyl (4-benzylphenyl)acetate 
• 1356067-61-2 (2R)-(-)-oxiran-2-ylmethyl 2-(4-benzylphenyl)acetate 
• 1356067-62-3 (2S)-(+)-oxiran-2-ylmethyl 2-(4-benzylphenyl)acetate 
• 1356067-64-5 2-hydroxy-1-(hydroxymethyl)ethyl 2-(4-benzylphenyl)acetate 
• 1356067-69-0 2-(benzyloxy)-1-[(benzyloxy)methyl]ethyl 2-(4-benzylphenyl)acetate 
• 35889-03-3 2-(4-benzylphenyl)acetic acid 

Relevant academic research and scientific papers

SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis

Monoacylglycerol lipase (MAGL) is the enzyme responsible for the inactivation of the endocannabinoid 2-arachidonoylglycerol (2-AG). MAGL inhibitors show analgesic and tissue-protecting effects in several disease models. However, the few efficient and selective MAGL inhibitors described to date block the enzyme irreversibly, and this can lead to pharmacological tolerance. Hence, additional classes of MAGL inhibitors are needed to validate this enzyme as a therapeutic target. Here we report a potent, selective, and reversible MAGL inhibitor (IC50 = 0.18 mm) which is active in vivo and ameliorates the clinical progression of a multiple sclerosis (MS) mouse model without inducing undesirable CB1-mediated side effects. These results support the interest in MAGL as a target for the treatment of MS.

Palladium-catalyzed and copper-mediated cross-coupling reaction of aryl- or alkenylboronic acids with acid chlorides under neutral conditions: Efficient synthetic methods for diaryl ketones and chalcones at room temperature

Palladium-catalyzed cross-coupling reaction of aryl- or alkenylboronic acids with acid chlorides in the presence of copper(I) thiophene-2-carboxylate (CuTC) as an activator in diethyl ether at room temperature under strictly non-basic conditions affords the diaryl ketones or chalcones in moderate to excellent yields. A wide range of substrates bearing an electron-donating or an electron-withdrawing substituent on the aromatic ring are compatible.

Structure-activity relationship of a new series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors

The two endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), play independent and nonredundant roles in the body. This makes the development of both selective and dual inhibitors of their inactivation an important priority. In this work we report a new series of inhibitors of monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH). Among them, (±)-oxiran-2-ylmethyl 6-(1,1′-biphenyl-4-yl)hexanoate (8) and (2R)-(-)-oxiran-2-ylmethyl(4-benzylphenyl)acetate (30) stand out as potent inhibitors of human recombinant MAGL (IC50 (8) = 4.1 μM; IC 50 (30) = 2.4 μM), rat brain monoacylglycerol hydrolysis (IC 50 (8) = 1.8 μM; IC50 (30) = 0.68 μM), and rat brain FAAH (IC50 (8) = 5.1 μM; IC50 (30) = 0.29 μM). Importantly, and in contrast to the other previously described MAGL inhibitors, these compounds behave as reversible inhibitors either of competitive (8) or noncompetitive nature (30). Hence, they could be useful to explore the therapeutic potential of reversible MAGL inhibitors.

Synthesis of α-Aryl nitriles through palladium-catalyzed decarboxylative coupling of cyanoacetate salts with aryl halides and triflates

Worth its salt: The palladium-catalyzed decarboxylative coupling of the cyanoacetate salt as well as its mono- and disubstituted derivatives with aryl chlorides, bromides, and triflates is described (see scheme). This reaction is potentially useful for the preparation of a diverse array of α-aryl nitriles and has good functional group tolerance. S-Phos=2-(2,6- dimethoxybiphenyl)dicyclohexylphosphine), Xant-Phos=4,5-bis(diphenylphosphino)- 9,9-dimethylxanthene. Copyright

Mild palladium-catalyzed selective monoarylation of nitriles

Two new palladium-catalyzed procedures for the arylation of nitriles under less basic conditions than previously reported have been developed. The selective monoarylation of acetonitrile and primary nitriles has been achieved using α-silyl nitriles in the presence of ZnF2. This procedure is compatible with a variety of functional groups, including cyano, keto, nitro, and ester groups, on the aryl bromide. The arylation of secondary nitriles occurred in high yield by conducting reactions with zinc cyanoalkyl reagents. These reaction conditions tolerated base-sensitive functional groups, such as ketones and esters. The combination of these two methods, one with a-silyl nitriles and one with zinc cyanoalkyl reagents, provides a catalytic route to a variety of benzylic nitriles, which have not only biological significance but utility as synthetic intermediates. The utility of these new coupling reactions has been demonstrated by a synthesis of verapamil, a clinically used drug for the treatment of heart disease, by a three-step route from commercial materials that allows convenient variation of the aryl group.

HETEROAROMATIC RING COMPOUNDS

Heteroaromatic ring compounds or pharmaceutically acceptable salts thereof, which have excellent characteristics and have strong curative effects to immuno-imbalance and choronic inflammation. Representative is the compound of the formula:

Photochemistry of benzophenone immobilized in a major groove of DNA: Formation of thermally reversible interstrand cross-link

We here report a highly site and sequence selective formation of an interstrand cross-link of BPU-containing oligomer duplexes. The cross-link was found spontaneously reverted to original oligomers upon heating, providing a new method for the temporary connection of two DNA strands. Copyright

Efficient photodecarboxylation of aroyl-substituted phenylacetic acids in aqueous solution: A general photochemical reaction

Photolysis (254-350 nm) of a variety of aroyl-substituted phenylacetic acids and p-acetylphenylacetic acid in aqueous solution at pH > pK(a) resulted in efficient photodecarboxylation (Φ = 0.2-0.7), to give in most cases a single product arising via the corresponding arylmethyl carbanion, indicating that photodecarboxylation is an efficient and general reaction for these types of compounds.

p-cyano substituted benzophenone as an excellent photophore for one- electron oxidation of DNA

Novel DNA-photocleaving molecule 1 consisting of a p-cyano substituted benzophenone photophore and an alkyl amino side chain was developed. DNA cleavage by 1 under photoirradiation conditions occurred selectively at 5' side G of 5'GG3' sequence after hot