Dedicated to Prof. Kwunmin ChenA sequential formal [4 + 2] cyclization involving cascade protocol has been developed for the construction of multisubstituted six-membered spirocyclic scaffolds by using 2arylidene-1, 3-indanedione and nitro allylic alcohol. This method generates four stereocenters in spiropyran ring with high diastereoselctivity (99 : 1) under mild reaction conditions.
Ulcerative colitis (UC) is a major clinical form of inflammatory bowel disease. UC is characterized by mucosal inflammation limited to the colon, always involving the rectum and a variable extent of the more proximal colon in a continuous manner. Genetic variations in DNA repair genes may influence the extent of repair functions, DNA damage, and thus the manifestations of UC. This study thus evaluated the role of polymorphisms of the genes involved in DNA repair mechanisms. A total of 171 patients and 213 controls were included. Genotyping was carried out by ARMS PCR and PCR-RFLP analyses for RAD51, XRCC3 and hMSH2 gene polymorphisms. Allelic and genotypic frequencies were computed in both control & patient groups and data was analyzed using appropriate statistical tests. The frequency of ‘A’ allele of hMSH2 in the UC group caused statistically significant increased risk for UC compared to controls (OR 1.64, 95% CI 1.16–2.31, p = 0.004). Similarly, the CT genotype of XRCC3 gene was predominant in the UC group and increased the risk for UC by 1.75 fold compared to controls (OR 1.75, 95% CI 1.15–2.67, p = 0.03), further confirming the risk of ‘T’ allele in UC. The GC genotype frequency of RAD51 gene was significantly increased (p = 0.02) in the UC group (50.3%) compared to controls (38%). The GC genotype significantly increased the risk for UC compared to GG genotype by 1.73 fold (OR 1.73, 95% CI 1.14–2.62, p = 0.02) confirming the strong association of ‘C’ allele with UC. Among the controls, the SNP loci combination of hMSH2:XRCC3 were in perfect linkage. The GTC and ACC haplotypes were found to be predominant in UC than controls with a 2.28 and 2.93 fold significant increase risk of UC.
The reaction of β‐naphthol with nitrostyrene derived primary MBH acetates in presence of Cs2CO3 as base resulted in the formation of 3‐nitro‐4‐phenyl‐3,4‐dihydro‐2H‐naphthopyran as the major isomer via SN2′ process. Due to the bis‐electrophilic nature of MBH acetates, the minor product 3‐nitro‐2‐phenyl‐3,4‐dihydro‐2H‐naphthopyran was also obtained presumably due to SN2 process with γ
‐attack on MBH acetates. The state of the art density functional theory (DFT) calculations were carried out to account for these competitive pathways towards the formation of major and minor products.
A simple and efficient cascade reactionviaformal [1+2+3] cyclization of 1,3‐indanedione, aldehyde and 2‐naphthol is reported using K2CO3as a base. The advantage includes metal‐free conditions, varied substrate scope and shortened reaction duration with high diastereoselectivity (i. e., 99 : 1) resulting in the formation of two carbon‐carbon as well as two carbon‐oxygen bonds through Knoevenagel‐Friedel‐Crafts‐Hemiketalization sequence resulting in three contiguous stereocenters.
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