355379-05-4

Upstream product

• 936130-82-4 methyl 4-(piperidine-4-yl)benzoate hydrochloride 
• 24424-99-5 di-tert-butyl dicarbonate 
• 619-42-1 4-methoxycarbonylphenyl bromide 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 619-44-3 methyl 4-iodobenzoate 
• 17763-71-2 4-carbomethoxyphenyl triflate 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 301673-14-3 tert-butyl 4-iodopiperidine-1-carboxylate 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 106047-17-0 4-Pyridin-4-yl-benzoic acid methyl ester 
• 99768-12-4 4-methoxycarbonylphenylboronic acid 
• 1120-87-2 4-bromopyridin 
• 281235-04-9 methyl 4-(piperidine-4-yl)benzoate 

Downstream Products

• 149353-75-3 4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid 
• 936130-82-4 methyl 4-(piperidine-4-yl)benzoate hydrochloride 

Relevant academic research and scientific papers

Chimeric compound for targeted degradation of androgen receptor protein, preparation method of chimeric compound and application of chimeric compound in medicine

The invention relates to a chimera compound for targeted degradation of androgen receptor protein, a preparation method of the chimera compound and application of the chimera compound in medicine. Specifically, the invention relates to a chimera (PROTAC) compound for targeted degradation of AR protein of a fused heterocyclic cerebellar protein (cerebellone) E3 ubiquitin ligase ligand as shown in a general formula (IM), a preparation method of the chimera compound, and application of the chimera compound in medicine, and particularly relates to a chimera (PROTAC) compound for targeted degradation of AR protein of a fused heterocyclic cerebellar protein E3 ubiquitin ligase ligand of a fused heterocyclic cerebellar protein E3 ubiquitin ligase ligand.

Photoinduced Nickel-Catalyzed Deaminative Cross-Electrophile Coupling for C(sp2)-C(sp3) and C(sp3)-C(sp3) Bond Formation

The construction of C-C bonds through cross-coupling between two electrophiles in the absence of excess metallic reducing agents is a desirable objective in chemistry. Here, we show that N-alkylpyridinium salts can be efficiently merged with aryl or alkyl halides in an intermolecular fashion, affording products in up to 92% yield at ambient temperature. These reactions harness the ability of N-alkylpyridinium salts to form electron donor-acceptor complexes with Hantzsch esters, enabling photoinduced single-electron transfer and fragmentation to afford alkyl radicals that are subsequently trapped by a Ni-based catalytic species to promote C(sp2)-C(sp3) and C(sp3)-C(sp3) bond formation. The operationally simple protocol is applicable to site-selective cross-coupling and tolerates diverse functional groups, including those that are sensitive toward metal reductants.

Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character

The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.

PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST

The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.

Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)

The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)

Alcohols as Latent Coupling Fragments for Metallaphotoredox Catalysis: Sp3-sp2 Cross-Coupling of Oxalates with Aryl Halides

Alkyl oxalates, prepared from their corresponding alcohols, are engaged for the first time as carbon radical fragments in metallaphotoredox catalysis. In this report, we demonstrate that alcohols, native organic functional groups, can be readily activated with simple oxalyl chloride to become radical precursors in a net redox-neutral Csp3-Csp2 cross-coupling with a broad range of aryl halides. This alcohol-activation coupling is successfully applied to the functionalization of a naturally occurring steroid and the expedient synthesis of a medicinally relevant drug lead.

An Improved System for the Aqueous Lipshutz-Negishi Cross-Coupling of Alkyl Halides with Aryl Electrophiles

The development of a palladacyclic precatalyst supported by a new biaryl(dialkyl)phosphine ligand (VPhos) in combination with octanoic acid/sodium octanoate as a simple and effective surfactant system provided an improved catalyst system for the rapid con

Single-electron transmetalation: An enabling technology for secondary alkylboron cross-coupling

Single-electron-mediated alkyl transfer affords a novel mechanism for transmetalation, enabling cross-coupling under mild conditions. Here, general conditions are reported for cross-coupling of secondary alkyltrifluoroborates with an array of aryl bromides mediated by an Ir photoredox catalyst and a Ni cross-coupling catalyst.

Alkylations of Arylboronic Acids including Difluoroethylation/Trifluoroethylation via Nickel-Catalyzed Suzuki Cross-Coupling Reaction

An efficient alkylation method of functionalized alkyl halides under mild nickel-catalyzed C(sp3)-(sp2) Suzuki cross-coupling conditions is described. The features of this approach are excellent functional group compatibility, low cost nickel catalyst, and the use of a mild base. This is also the first successful example of the nickel-catalyzed direct 2,2-difluoroethylation or 2,2,2-trifluoroethylation of aryl-/heteroarylboronic acids.

BENZAMIDE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER

The present invention is directed to benzamide derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, liver related disorders and viral infections. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, (II) and (III) are defined herein.