Our study focussed the synthesis and rest of the activity studies

Our study focussed the synthesis and rest of the activity studies is under progress. (Scheme 1). In the synthesis of Int-1, we have used some earlier patented work.17 The cyclised ester (3) was prepared by Cyclisation of ethyl di bromopropionate (1) with pyrocatechol (2) in anhy. acetone. The cyclised ester (3) hydrolysed using NaOH in ethanol and water to afford acid (4).18 The acid (4) converted to acid chloride (5) using oxallyl chloride and further coupled with piperzine in present of sodium acetate and further followed pH adjustments to afford Int-1 according to (Scheme 2). The compound 2,3-Dichlorophenylpiperazine (2,3-DCPP) FRAX597 (Int-2) well known intermediate

in the synthesis of aripiprazole and one of its metabolites.19 and 20 This is prepared by cyclisation of 2,3-dichloro aniline BTK inhibitor (7) with dichloro ethyl amine (8) using aq.HCl to afford (2,3-DCPP) (Int-2) according to (Scheme 3). The choro (9) and (10) using POCl3 as a chlorinating reagent to afford choro compound (10)

and (15). The further traditional approach for the synthesis21 of (Int-3) to (Int-7) as shown in Scheme 4. The conversion of nitro compounds (9) and (14) to corresponding conversation of choro compounds (10), (15) and (26) into (11), (16), (19), (22), and (27) using appropriate alcohols, the methylation of compound (25) using DMS to afford methylated compound (26). The further conversion of compounds, (11), (16), (19), (22), (24) & (29) to acetate using acetic anhydride to afford compounds, (12), (17), (20), (23), and (28). These all these compounds further hydrolysed NaOH to offered (13), (18), (21) and (27). Finally chlorinated all these compounds using SOCl2 under similar reaction condition to afford (Int-3) to (Int-7) according to Scheme 4.21 and 22 The Novel targets (SLN1–SLN10) were synthesized by simple coupling using different technologies (microwave, ultra-sonication and normal conventional method). Basically, we observed Ultra-Sonication condition looking better comparatively with other techniques

used based on CYTH4 yield reported in Table 1. All the reactions routinely monitored by Thin-layer chromatography (TLC) using Merck silica gel 60 F254 coated aluminium plates using several solvent systems of different polarity. The following mobile phases were employed ethylacetae/hexane, ethylacetate/dichloromethane, methanol/dichloromethane and methanol-ethyl acetate with different percentage combinations. The Column chromatography by using all vensil columns are used for purification of compounds used (60–120 mesh) silica-gel. The Melting points were determined in open capillaries on a Thermonick melting point apparatus and found uncorrected. 1H NMR (400 MHz) and 13C NMR (100 MHz) recorded on CDCl3 and DMSO-d6 solution in a 5 mm tube on Varian 400 MHz Unity Inova using TMS internal reference standard (chemical shifts in δ).Mass spectra were recorded on Agilent 6310 Ion Trap and Shimadzu LCMS (e/z and relative intensity).

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