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A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a–5l) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the in situ generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by 1H NMR, 13C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for in vitro antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound N-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1-yl)sulfonyl)phenyl) acetamide (5l) was found to exhibit potent activity as compared to the standard drugs.

S,S- and S,S,S-substituted nitrodienes 3a, 3b, and 4a were synthesized by reactions of 1,1,2,4,4-pentachloro-3-nitro-1,3-butadiene with some thiols 4-chlorobenzylmercaptan and 2-chlorobenzylmercapt...

Thiomorpholine 1,1-dioxides were prepared with double Michael addition reaction of aromatic amines to divinyl sulfone catalyzed by boric acid / glycerol in water. This catalyst system was also used for the Michael addition reaction of aromatic amines to electron-deficient alkenes. The reaction is simple and green and gives good to excellent yields.

The novel S-, S,S-, and S,S,S-substituted nitrobutadienes were synthesized from the reactions of 2-nitrobutadiene compounds with some thiols. The new N,S-substituted nitrobutadienes were obtained from the reaction of the mono-thiosubstituted butadienes with morpholine, thiomorpholine, homopiperazine, and piperazine derivatives. The structures of new compounds were determined by spectroscopic techniques. GRAPHICAL ABSTRACT

Thirteen new stannacyclododecane dithiocarbamate complexes have been prepared by reacting 12-chloro-12-n-butyl-1,11-dioxa-4,8-dithia-12-stannacyclododecane (1) and 12-chloro-12-n-butyl-1,4,8,11-tetrathia-12-stannacyclododecane (2) with pyrrolidine-, morpholine-, thiomorpholine-, piperidine-, piperazinebis-, and 3-pyrroline-carbodithioates, respectively, as well as with diethyl-dithiocarbamate. All complexes were characterized by elemental analyses, IR, EI-MS, and NMR (1H, 13C, and 119Sn) studies. The spectroscopic data suggest the replacement of the chlorides by the corresponding dithiocarbamates with monodentate coordination, leading to six-coordinate tin atoms in all the cases.

N,S-Substituted nitrobutadienes 3a–g were synthesized from the reaction of the thiosubstituted derivatives 1a–g with thiomorpholine 2. The N,S-substituted nitrobutadienes 5a–g were obtained from the reaction of the thiosubstituted butadienes 1a–g with N-diphenylmethyl piperazine 4. The structure of butadiene 3c was elucidated by single crystal X-ray diffraction.

Interaction of dapson [bis(4-aminophenyl)sulfone] 1 with [bis-(methylsulfonyl) methylidine]malononitrile 2 yielded the corresponding dicyano derivative 3, which was reacted with acetic anhydride, succinic anhydride, 4-chlorobenzaldehyde, phenyl isothiocyanate to give the corresponding acetamide 4, succinamic acid 5, pyrrolidine 6, Shiff base 7 and thiourea 8, respectively. Treatment of 3 with chloroacetyl chloride afforded the aminoacetyl chloride derivative 9. Further, the interaction of compound 9 with thioglycolic acid, malononitrile, ethyl glycinate hydrochloride, and/or potassium thiocyanate furnished compounds 10–15, respectively. The structural characterization of the prepared compounds was based on microanalytical and spectroscopic analyses. Some of the prepared compounds were tested for their antimicrobial and antitumor activities. Compounds 9 and 12 showed promising antitumor activity compared with Doxorubicin as positive control.

Compound 3 and 5a, b were obtained from the reaction of 1,3,4,4-tetrachloro-1-thioallyl-2-nitro-1,3-butadiene (1) with thiomorpholine (2) and piperazine derivatives 4a, b in dichloromethane. The reaction of compound 1 and bromine gave compound 6. Compounds 8 and 10 were obtained from the reaction of 6 with 1-(diphenylmethyl)piperazine (7) and piperidine (9) in dichloromethane. The derivative 13 was synthesized from the reaction of 4-bromo-1,1,3,4-tetrachloro-2-nitro-1,3-butadiene (11) and allylmercaptane (12). Compounds 15 and 16a, b were obtained from the reaction of 1-allyl-4-bromo-1,3,4-trichloro-2-nitro-1,3-butadiene (13) with morpholine (14) and the piperazine derivatives 16a, b, in dichloromethane, respectively.

The substituted 1,2-dibromomethanethio nitrodiene 2 was obtained from the addition of bromine to S-substituted nitrodien 1 in carbon tetrachloride. N, S-substituted compounds 4a–h were synthesized from the reactions of compound 2 with several substituted piperazine derivatives 3a–h in dichloromethane. N, S-substituted compounds 6 and 8 were synthesized from the reaction of 2 with morpholine ( 5 ) and thiomorpholine ( 7 ) in dichloromethane, respectively. Dibutadienyl piperazines 10 , 12 , and 14 were synthesized from the reactions of 2 with homopiperazine ( 9 ), piperazine ( 11 ), and 2,5-dimethylpiperazine ( 13 ), respectively.

Being used for the extraction from an aqueous to an organic phase thiomorpholine substituted all-homo-calix[6]arene 1 turns out to be more efficient and much more selective for Pd11 than the corresponding calix[6]arene 2 and a comparable open-chained compound 3.