41420-77-3Relevant academic research and scientific papers
AgNO3Catalyzed Regio-Selective Synthesis of 3-Alkyl/Aryl-idene-3,4-dihydro-4-tosyl-2H-1,4-Benzoxazine: Novel Anti-Tubercular Scaffolds
Karunanidhi, Sivanandhan,Karpoormath, Rajshekhar,Bera, Milan,Rane, Rajesh A.,Palkar, Mahesh B.
, p. 1611 - 1616 (2016)
A facile and efficient method for the construction of 3-alkyl/aryl substituted 1,4-benzoxazine and benzoxazepine via AgNO3catalyzed cyclization of propargyloxy sulfonamides and their anti-tubercular activity against Mycobacterium tuberculosis H37RVis described. This cyclization proceeds through 6-exo-dig manner to generate the products in moderate to good yields.
Method for synthesizing 2-benzyl-1,5-dihydrobenzo[e][1,4]oxazepine in multiple steps
-
Paragraph 0067; 0068, (2018/12/02)
The invention discloses a method for synthesizing (E)-2-benzal-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine in multiple steps, and belongs to the technical field of organic synthesis. Aethrization of o-nitrobenzyl alcohol and propargyl bromide or propargyl alcohol is performed to obtain 1-nitro-2-(propynyloxymethyl)-benzene, the 1-nitro-2-(propynyloxymethyl)-benzene is reduced by iron powder / aceticacid or NiCl2 (dppp) / tetrahydroxy diborane/organic base to obtain 2-(propynyloxymethyl)-aniline, the 2-(propynyloxymethyl)-aniline is coupled with iodobenzene by Sonogashira to obtain 2-[(3-phenyl-2-alkynyloxy)methyl]anilide, and the (E)-2-benzal-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine is obtained by acetyl protection of amino group, ring closure by cuprous bromide / cesium carbonate and deprotection under basic conditions.
Method for synthesizing (E)-2-benzal-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine in multiple steps
-
Paragraph 0067; 0068, (2018/12/02)
The invention discloses a method for synthesizing (E)-2-benzal-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine in multiple steps, and belongs to the technical field of organic synthesis. Aethrization of o-nitrobenzyl alcohol and propargyl bromide or propargyl alcohol is performed to obtain 1-nitro-2-(propynyloxymethyl)-benzene, the 1-nitro-2-(propynyloxymethyl)-benzene is reduced by iron powder / aceticacid or NiCl2 (dppp) / tetrahydroxy diborane/organic base to obtain 2-(propynyloxymethyl)-aniline, the 2-(propynyloxymethyl)-aniline is coupled with iodobenzene by Sonogashira to obtain 2-[(3-phenyl-2-alkynyloxy)methyl]anilide, and the (E)-2-benzal-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine is obtained by benzoyl protection of amino group, ring closure by cuprous bromide / cesium carbonate and deprotection under basic conditions.
Method for synthesizing (E)-2-benzylidene-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine
-
Paragraph 0060; 0061; 0067; 0068, (2019/01/08)
The invention discloses a method for synthesizing (E)-2-benzylidene-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine by multiple steps, and belongs to the technical field of organic synthesis. The method comprises the following steps: 2-nitrobenzyl alcohol and propargyl bromide or propargyl alcohol are subjected to ether formation, and 1-nitro-2-(propynyloxymethyl)-benzene is obtained; then, reduction isperformed with iron powder/acetic acid or NiCl2(dppp)/tetrahydroxydiboron/organic base, and 2-(propynyloxymethyl)-aniline is obtained; 2-(propynyloxymethyl)-aniline is subjected to Sonogashira coupling with iodobenzene, and 2-[(3-phenyl-2-alkynyloxy)methyl]-aniline is obtained; amino is subjected to p-toluenesulfonyl protection, cuprous bromide/cesium carbonate ring closing is performed, deprotection is performed under the condition of metal sodium/naphthalene, and (E)-2-benzylidene-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine is obtained.
Multi-step synthesis method for 2-benzyl-1,5-dihydrobenzo[e][1,4]oxazepine
-
Paragraph 0067; 0068, (2019/01/08)
The invention discloses a multi-step synthesis method for 2-benzyl-1,5-dihydrobenzo[e][1,4]oxazepine, and belongs to the technical field of organic synthesis. The method comprises the following steps:2-nitrobenzyl alcohol and propargyl bromide or propargyl alcohol are used for ether formation, and 1-nitro-2-(propynyloxymethyl)-benzene is obtained; then, reduction is performed with iron powder/acetic acid or NiCl2 (dppp)/tetrahydroxydiboron/organic base, and 2-(propynyloxymethyl)-aniline is obtained; 2-(propynyloxymethyl)-aniline is subjected to Sonogashira coupling with iodobenzene, and 2-[(3-phenyl-2-alkynyloxy)methyl]-aniline is obtained; amino is subjected to p-toluenesulfonyl protection, cuprous bromide/cesium carbonate ring closing is performed, deprotection is performed under the condition of metal sodium/naphthalene, and 2-benzyl-1,5-dihydrobenzo[e][1,4]oxazepine is obtained.
The multi-step synthetic 2 - benzyl - 1, 5 - dihydrobenzo [e] [1, 4] oxygen nitrogen mixed outstanding method (by machine translation)
-
Paragraph 0060-0068, (2018/12/02)
The present invention discloses a multi-step synthesis of 2 - benzyl - 1, 5 - dihydrobenzo [e] [1, 4] method of oxygen nitrogen mixed outstanding, which belongs to the technical field of organic synthesis. The O-nitryl animal pen or methylacetylene [...] obtained alcohol and 1 - nitro - 2 - (propynyl ethoxymethyl) - benzene, then adopts iron powder/acetic acid or NiCl2 (dppp)/tetrahydroxy boron/organic base reduction to obtain 2 - (propynyl ethoxymethyl) - aniline, subsequently with the occurrence obtained by coupling the Sonogashira oxygenated esters of 2 - [(3 - phenyl - 2 - [...]) methyl] - aniline, then the amino benzoyl protection after carried out, through the cuprous bromide/[...] carbonate, followed by deprotection under alkaline conditions to obtain the 2 - benzyl - 1, 5 - dihydrobenzo [e] [1, 4] oxygen nitrogen mixed outstanding. (by machine translation)
