2-Bromo-5-methanesulfonylthiophene → [2-Fluoro-4-(5-methanesulfonyl-thiophen-2-yl)-phenyl]-[2-(S)-(2-(R)-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-methanone

Participants

Role	Name	HCID	Charge
Reactant	2-Bromo-5-methanesulfonylthiophene	HCID 17390281	—
Reactant	2-Fluoro-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl[2-(S)-(2-(R)-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-methanone	HCID 57980040	—
Product	[2-Fluoro-4-(5-methanesulfonyl-thiophen-2-yl)-phenyl]-[2-(S)-(2-(R)-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-methanone	HCID 59264696	78%

Reaction Steps

The title compound is prepared in a manner substantially analogous to General Procedure A using [2-Fluoro-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-[2-(S)-(2-(R)-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-methanone (458 mg, 1.1 mmol) and 2-Bromo-5-methanesulfonyl-thiophene (CAS 2160-61-4) (255 mg, 1.0 mmol) to give 350 mg (78% yield). MS (ES+) 451.2 (M+H)+

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US07705025B2
Source dataset	uspto-grants-2010_04
ORD ID	ord-4b73507070094a359e229cd324291074
Source note	uspto-grants-2010_04