106191-02-0Relevant articles and documents
Multi-gram synthesis of enantiopure 1,5-disubstituted tetrazoles via Ugi-azide 3-component reaction
Capurro, Pietro,Moni, Lisa,Galatini, Andrea,Mang, Christian,Basso, Andrea
, (2018)
Tetrazoles have been widely studied for their biological properties. An efficient route for large-scale synthesis of 1,5-disubstituted tetrazoles (1,5-DTs) is presented. The strategy exploits a reductive approach to synthetize a cyclic chiral imine substrate which is then converted into the target product through an Ugi-azide three-component reaction (UA-3CR). The final products are equipped with additional functionalities which can be further elaborated for the generation of combinatorial libraries of enantiopure heterocycles.
Zr-mediated synthesis of chiral cyclic imines and their application in Betti reactions
Speich, Elena,Banfi, Luca,Moni, Lisa,Riva, Renata,Rocca, Valeria,Basso, Andrea
, p. 329 - 333 (2018)
[Figure not available: see fulltext.] A novel synthetic strategy has been outlined to assemble enantiomerically pure Betti bases with unprecedented structures. This involves the Zr-mediated reduction of pyrrolidin-2-ones to cyclic imines and their subsequent reaction with phenolic derivatives.
A cascade strategy enables a total synthesis of (-)-gephyrotoxin
Chu, Shuyu,Wallace, Stephen,Smith, Martin D.
, p. 13826 - 13829 (2014)
A concise and efficient synthesis of (-)-gephyro-toxinfrom L-pyroglutaminol has been realized. The key step in this approach is a diastereoselective intramolecular enamine/ Michael cascade reaction that forms two rings and two stereocenters and generates a stable tricyclic iminium cation. A hydroxy-directed reduction of this intermediate plays a key role in establishing the required cis-decahydroquinoline ring system, enabling the total synthesis of (-)-gephyrotoxin in nine steps and 14 % overall yield. The absolute configuration of the synthetic material was confirmed by single-crystal X-ray diffraction and is consistent with the structure originally proposed for material isolated from the natural source.
BTK inhibitors containing 4-azaspiro heptane
-
Paragraph 0088-0091, (2021/01/24)
The invention belongs to the field of medicinal chemistry, and relates to a BTK inhibitor containing 4-azaspiro heptane, in particular to a compound shown as a formula(I)or pharmaceutically acceptablesalt thereof, a preparation method of the compound, a pharmaceutical composition containing the compound, and application of the compound to treatment of BTK related diseases.
Diastereoselective Diboration of Cyclic Alkenes: Application to the Synthesis of Aristeromycin
Vendola, Alex J.,Allais, Christophe,Dechert-Schmitt, Anne-Marie R.,Lee, James T.,Singer, Robert A.,Morken, James P.
supporting information, p. 2863 - 2867 (2021/05/05)
The Pt-catalyzed diboration of cyclic alkenes is extended to unsaturated heterocycles and bicyclic compounds and can be accomplished in a diastereoselective fashion. The optimal procedures, substrate scope, and diastereoselectivity were investigated, and examples employing both homogeneous and heterogeneous catalysis were examined. Lastly, application to the construction of the nucleoside analog (±)-aristeromycin was conducted.
N-Heterocyclic carbene triazolium salts containing brominated aromatic motifs: Features and synthetic protocol
Raed, Anas Abo,Dhayalan, Vasudevan,Barkai, Shahar,Milo, Anat
, p. 878 - 882 (2020/12/25)
In this work, we provide a brief overview of the role of N-aryl substituents on triazolium N-heterocyclic carbene (NHC) catalysis. This synopsis provides context for the disclosed synthetic protocol for new chiral N-heterocyclic carbene (NHC) triazolium salts with brominated aromatic motifs. Incorporating brominated aryl rings into NHC structures is challenging, probably due to the substantial steric and electronic influence these substituents exert throughout the synthetic protocol. However, these exact characteristics make it an interesting N-aryl substituent, because the electronic and steric diversity it offers could find broad use in organometallic- A nd organo-catalysis. Following the synthetic reaction by NMR guided the extensive modification of a known protocol to enable the preparation of these challenging NHC pre-catalysts.
FUSED RING COMPOUNDS
-
Paragraph 0717, (2020/06/01)
This invention pertains to fused ring compounds of Formula (I), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.
HETEROARYL(HETEROCYCLYL)METHANOL COMPOUNDS USEFUL IN THE TREATMENT OF HYPERGLYCAEMIA
-
Page/Page column 53, (2020/10/09)
There is herein provided a compound of formula I (I) or a pharmaceutically acceptable salt thereof, wherein the ring comprising Q1 to Q5, R1, m, X1 and ring A have meanings as provided in the description.
INHIBITORS OF APOL1 AND METHODS OF USING SAME
-
Paragraph 00313, (2020/07/14)
The disclosure provides at least one entity chosen from compounds of formula (I), solid state forms of the same, compositions comprising the same, and methods of using the same, including use in treating focal segmental glomerulosclerosis (FSGS) and/or non-diabetic kidney disease (NDKD).
HETEROCYCLYL(PHENYL)METHANOL COMPOUNDS USEFUL IN THE TREATMENT OF HYPERGLYCAEMIA
-
Page/Page column 44; 53, (2020/10/09)
There is herein provided a compound of formula I or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, ring A, n and y have meanings as provided in the description.