1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine

Base Information

• Chemical Name: 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine
• CAS No.: 1608469-50-6
• Molecular Formula: C₂₀H₂₃F₃N₂O₄S
• Molecular Weight: 443.476

Synonyms:1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine

Chemical Property of 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine

Chemical Property:

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Technology Process of 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine

There total 9 articles about 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[¹⁸F]fluoroethyl)piperazine which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

4-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)piperazine + [(18)F]-2-fluoroethyltosylate (113426-12-3) → 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[18F]fluoroethyl)piperazine (1608469-50-6)

Guidance literature:

With sodium carbonate; In acetonitrile; at 150 ℃; for 0.166667h; Solvent; Microwave irradiation;

Reference yield:

4-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)piperazin-1-ium chloride + [(18)F]-2-fluoroethyltosylate (113426-12-3) → 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[18F]fluoroethyl)piperazine (1608469-50-6)

Guidance literature:

In dimethyl sulfoxide; at 140 ℃; for 0.5h; Sealed tube;

Reference yield:

tert-butyl 4-(5-amino-2-methoxyphenyl)piperazine-1-carboxylate (148546-91-2) → 1-(5-(3-(difluoromethoxy)phenylsulfonyl)-2-methoxyphenyl)-4-(2-[18F]fluoroethyl)piperazine (1608469-50-6)

Guidance literature:

Multi-step reaction with 4 steps

1.1: trifluoroacetic acid / dichloromethane / 0 °C

1.2: 0.17 h / 0 °C

1.3: 2 h / 0 - 5 °C

2.1: caesium carbonate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; tris-(dibenzylideneacetone)dipalladium⁽⁰⁾; tetrabutyl-ammonium chloride / toluene / 8 h / 80 °C / Inert atmosphere

3.1: hydrogenchloride / ethanol; isopropyl alcohol / 20 °C

4.1: dimethyl sulfoxide / 0.5 h / 140 °C / Sealed tube

With hydrogenchloride; tris-(dibenzylideneacetone)dipalladium⁽⁰⁾; tetrabutyl-ammonium chloride; caesium carbonate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; trifluoroacetic acid; In ethanol; dichloromethane; dimethyl sulfoxide; isopropyl alcohol; toluene;

upstream raw materials:

1,2-bis-tosyloxyethane

[(18)F]-2-fluoroethyltosylate

tert-butyl 4-(2-methoxy-5-nitrophenyl)piperazine-1-carboxylate

tert-butyl 4-(5-amino-2-methoxyphenyl)piperazine-1-carboxylate

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