Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 540221Generated: October 29, 2026

trans-4-Fluoropyrrolidin-3-amine;dihydrochloride → trans-4-Fluoro-1-[6-methyl-2-(1-oxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)quinazolin-4-yl]pyrrolidin-3-amine

https://huagongshe.com/reaction/540221

Reaction equation

Participants

RoleNameHCIDCharge
Reactanttrans-4-Fluoropyrrolidin-3-amine;dihydrochlorideHCID 14612505—
Reactant2,3,4,5-Tetrahydrobenzo[f][1,4]thiazepine 1-oxideHCID 19608203—
Reactant2-Chloro-6-methyl-3,4-dihydroquinazolin-4-oneHCID 135588790—
Producttrans-4-Fluoro-1-[6-methyl-2-(1-oxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)quinazolin-4-yl]pyrrolidin-3-amineHCID 86691411—

Reaction Steps

The title compound was prepared in analogy to Example 62-1 in Scheme 23 by using 2-chloro-6-methylquinazolin-4(3H)-one, 2,3,4,5-tetrahydro-1,4-benzothiazepine 1-oxide and trans-4-fluoropyrrolidin-3-amine. MS obsd. (ESI+) [(M+H)+] 426. 1H NMR (400 MHz, CD3OD) 7.82 (s, 1 H), 7.71 (d, J=6.8 Hz, 1 H), 7.42 (m, 4 H), 5.26 (d, J=15.2 Hz, 1 H), 5.07 (d, J=51.2 Hz, 1 H), 4.78 (brs, 1 H), 4.43 (m, 2 H), 4.29 (m, 1 H), 4.06 (t, J=11.2 Hz, 1 H), 3.86 (d, J=12 Hz, 1 H), 3.75 (m, 1 H), 3.40 (m, 2 H), 2.40 (s, 3 H).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08871756B2
Source datasetuspto-grants-2014_10
ORD IDord-cb518493d42548158b1bbdc295966444
Source noteuspto-grants-2014_10