732275-93-3Relevant academic research and scientific papers
3-(5-METHOXY-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
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, (2021/06/26)
The present disclosure relates to compounds of formula (I') and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
PIPERIDINYL AMINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 25, (2021/04/03)
The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and co
Photoinduced Nickel-Catalyzed Deaminative Cross-Electrophile Coupling for C(sp2)-C(sp3) and C(sp3)-C(sp3) Bond Formation
Koh, Ming Joo,Wei, Yi,Yang, Tao
, p. 6519 - 6525 (2021/06/25)
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.
Ni-catalyzed Reductive Deaminative Arylation at sp3 Carbon Centers
Martin-Montero, Raul,Yatham, Veera Reddy,Yin, Hongfei,Davies, Jacob,Martin, Ruben
, p. 2947 - 2951 (2019/04/30)
A Ni-catalyzed reductive deaminative arylation at unactivated sp3 carbon centers is described. This operationally simple and user-friendly protocol exhibits excellent chemoselectivity profile and broad substrate scope, thus complementing existing metal-catalyzed cross-coupling reactions to forge sp3 C-C linkages. These virtues have been assessed in the context of late-stage functionalization, hence providing a strategic advantage to reliably generate structure diversity with amine-containing drugs.
Pd-PEPPSI-IPent-SiO2: A Supported Catalyst for Challenging Negishi Coupling Reactions in Flow
Price, Gregory A.,Hassan, Abbas,Chandrasoma, Nalin,Bogdan, Andrew R.,Djuric, Stevan W.,Organ, Michael G.
supporting information, p. 13347 - 13350 (2017/10/17)
A silica-supported precatalyst, Pd-PEPPSI-IPent-SiO2, has been prepared and evaluated for its proficiency in the Negishi cross-coupling of hindered and electronically deactivated coupling partners. The precatalyst Pd-PEPPSI-IPent loaded onto packed bed columns shows high catalytic activity for the room-temperature coupling of deactivated/hindered biaryl partners. Also for the first time, the flowed Csp3–Csp2 coupling of secondary alkylzinc reagents to (hetero)aromatics has been achieved with high selectivity with Pd-PEPPSI-IPent-SiO2. These couplings required residence times as short as 3 minutes to effect completion of these challenging transformations with excellent selectivity for the nonrearranged product.
PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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Paragraph 0097; 0101, (2017/07/29)
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.
Alcohols as Latent Coupling Fragments for Metallaphotoredox Catalysis: Sp3-sp2 Cross-Coupling of Oxalates with Aryl Halides
Zhang, Xiaheng,MacMillan, David W.C.
, p. 13862 - 13865 (2016/11/06)
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.
Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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Page/Page column 43; 44; 51; 52, (2017/07/31)
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)
Pd-PEPPSI-IPentCl: A highly effective catalyst for the selective cross-coupling of secondary organozinc reagents
Pompeo, Matthew,Hadei, Niloufar,Organ, Michael G.,Froese, Robert D. J.
, p. 11354 - 11357,4 (2012/12/12)
No migration? No problem. A series of new N-heterocyclic carbene based Pd complexes has been created and evaluated in the Negishi cross-coupling of aryl and heteroaryl chlorides, bromides, and triflates with a variety of secondary alkylzinc reagents (see scheme). The direct elimination product is nearly exclusively formed; in most examples there is no migratory insertion at all. Copyright
Pd-PEPPSI-IPentCl: A highly effective catalyst for the selective cross-coupling of secondary organozinc reagents
Pompeo, Matthew,Froese, Robert D. J.,Hadei, Niloufar,Organ, Michael G.
, p. 11354 - 11357 (2013/01/15)
No migration? No problem! A series of new N-heterocyclic carbene based Pd complexes has been created and evaluated in the Negishi cross-coupling of aryl and heteroaryl chlorides, bromides, and triflates with a variety of secondary alkylzinc reagents (see scheme). The direct elimination product is nearly exclusively formed; in most examples there is no migratory insertion at all. Copyright
