17549-79-0

Upstream product

• 51-66-1 4-methoxyacetanilide 
• 94299-05-5 N-(2-benzoyl-4-methoxyphenyl)acetamide 
• 104-94-9 4-methoxy-aniline 
• 100-47-0 benzonitrile 
• 6705-03-9 2-Amino-5-methoxybenzoic acid 
• 37795-77-0 6-methoxy-2H-3,1-benzoxazine-2,4(1H)-dione 
• 214971-09-2 2-amino-5,N-dimethoxy-N-methylbenzamide 
• 108-86-1 bromobenzene 

Downstream Products

• 924279-42-5 3-amino-7-methoxy-5-phenyl-1,3-dihydrobenzo[e][1,4]diazepin-2-one 
• 926888-10-0 (7-methoxy-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamic acid benzyl ester 
• 91409-69-7 2-(2-Benzoyl-4-methoxy-phenylamino)-propionic acid 
• 61085-29-8 7-benzoyl-5-methoxyindolin-2-one 
• 91713-65-4 7-Benzoyl-5-methoxy-3-methylsulfanyl-1,3-dihydro-indol-2-one 
• 61941-55-7 sodium 2-amino-3-benzoyl-5-methoxyphenylacetate 
• 42211-96-1 C₁₇H₁₉NO₂ 
• 1315314-52-3 6-methoxy-2,4-diphenylquinazoline 
• 1315477-60-1 5-methoxy-3-phenyl-1-tosyl-1H-indole-2-carbaldehyde 
• 1315477-42-9 1-(5-methoxy-2-(tosylamino)phenyl)-1-phenylprop-2-yn-1-ol 
• 1300089-42-2 benzyl (7-methoxy-5-phenyl-2-thioxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamate 
• 1300087-07-3 benzyl (8-methoxy-1-methyl-6-phenyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)carbamate 
• 1597443-29-2 (2-amino-5-methoxyphenyl)phenylmethanone oxime 
• 13097-05-7 5-methoxy-3-phenyl-1H-indazole 

Relevant academic research and scientific papers

Asymmetric Synthesis of Hydroquinazolines Bearing C4-Tetrasubstituted Stereocenters via Kinetic Resolution of α-Tertiary Amines

A novel protocol for asymmetric synthesis of hydroquinazolines bearing C4-tetrasubstituted stereocenters has been achieved through kinetic resolution of 2-amido α-tertiary benzylamines via chiral phosphoric acid catalyzed intramolecular dehydrative cyclizations. This method gave access to both α-tertiary benzylamines and hydroquinazolines with broad scope and high enantioselectivities. An intriguing restricted rotation of the C-N bond was observed for hydroquinazoline products bearing C4-tetrasubstituted stereocenters.

Pd-catalyzed regiodivergent synthesis of diverse oxindoles enabled by the versatile heck reaction of carbamoyl chlorides

We report herein a miscellaneous oxindole synthesis bearing an all-carbon quaternary center, enabled by Pd-catalyzed intramolecular cyclization followed by multiple intermolecular Heck reactions of both easily accessible alkene-tethered carbamoyl chlorides and olefins. This protocol obviates the use of prefunctionalized olefinic reagents, exhibits excellent functional group tolerance, and features fascinating reactive versatility.

Visible Light Induced Cyclization to Spirobi[indene] Skeletons from Functionalized Alkylidienecyclopropanes

In this paper, we revealed a metal-free and visible light photoinduced method for the rapid construction of spirobi[indene] skeletons, providing a simple and efficient way for easy access to spirobi[indene] scaffolds under mild conditions along with a broad substrate scope and good functional group tolerance.

Synthesis of Diiodinated All-Carbon 3,3′-Diphenyl-1,1′-spirobiindene Derivatives via Cascade Enyne Cyclization and Electrophilic Aromatic Substitution

A synthetic method for the construction of diiodinated all-carbon spirobiindene derivatives has been developed from the reaction of propargyl alcohol-tethered alkylidenecyclopropanes with iodine. The reaction proceeded through an iodination-initiated cascade intramolecular enyne cyclization and electrophilic aromatic substitution reaction process in 1,2-dichloroethane upon heating, giving desired spirocyclic products in moderate to excellent yields. Further transformation of the obtained products has also been presented.

Palladium-Catalyzed Cascade Reductive and Carbonylative Cyclization of Ortho-Iodo-Tethered Methylenecyclopropanes (MCPs) Using N-Formylsaccharin as CO Source

A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.

Lewis or Br?nsted acid-catalysed reaction of propargylic alcohol-tethered alkylidenecyclopropanes with indoles and pyrroles for the preparation of polycyclic compounds tethered with indole or pyrrole motif

We developed a facile synthetic method to access cyclopenta[b]naphthalene derivatives via the Lewis or Br?nsted acid catalysed cascade nucleophilic addition, electronic cyclization, ring-opening rearrangement of propargylic alcohol-tethered alkylidenecyclopropanes with indole and pyrrole derivatives. The reaction exhibited a broad substrate scope and good functional group tolerance under metal-free conditions, affording the desired products in moderate to good yields.

ORGANIC COMPOUNDS TO TREAT HEPATITIS B VIRUS

The disclosure relates to compositions comprising a HBV RNAi agent. In some embodiments, the HBV RNAi agent comprises a sense and an anti-sense strand, each strand being an 18-mer and the strands together forming a blunt-ended duplex, wherein the 3′ end of at least one strand terminates in a phosphate or modified internucleoside linker and further comprises, in 5′ to 3′ order: a spacer; a second phosphate or modified internucleoside linker; and a 3′ end cap. In some embodiments, the 3′ end of both the sense and anti-sense strand further comprise, in 5′ to 3′ order: a spacer; a second phosphate or modified internucleoside linker; and a 3′ end cap. The two strands can have the same or different spacers, phosphates or modified internucleoside linkers, and/or 3′ end caps. The strands can be ribonucleotides, or, optionally, one or more nucleotide can be modified or substituted. Optionally, at least one nucleotide comprises a modified internucleoside linker. Optionally, the RNAi agent can be modified on one or both 5′ end. Optionally, the sense strand can comprise a 5′ end cap which reduces the amount of the RNA interference mediated by this strand. Optionally, the RNAi agent is attached to a ligand. This format can be used to devise RNAi agents to a variety of different targets and sequences. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference. The disclosure also pertains to methods of treating, ameliorating and preventing HBV in a patient involving the step of administering to the patient a therapeutic amount of a HBV RNAi agent.

3'END CAPS FOR RNAi AGENTS FOR USE IN RNA INTERFERENCE

The disclosure relates to novel compounds and compositions comprising a RNAi agent comprising a novel compound as a 3' end cap. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference.

A mild and practical procedure for synthesis of substituted 2-aminobenzophenones

Abstract A convenient three-step procedure has been developed for synthesis of substituted 2-aminobenzophenones from substituted anilines. The anilines are first protected as acetanilides, by reaction with acetic anhydride. These are then benzoylated with (trichloromethyl)benzene in the presence of aluminium-generated 2-acetamidobenzophenone. Finally, removal of the acetyl group from the amino group provides the substituted 2-aminobenzophenones in moderate to good yields.

N-SUBSTITUTED BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH INHIBITORS

Disclosed are compounds of Formula (I): wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CF3, or -CH2CH2CH2CF3; R3 is -CH