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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 43805Generated: October 25, 2026

Methanol → Methyl cis(+/-)-2-(acetylamino)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoate

https://huagongshe.com/reaction/43805

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethanolHCID 887—
ReactantAcetyl chlorideHCID 6367—
ReactantTriethylamineHCID 8471—
ReactantMethyl cis(+/-)-2-amino-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoateHCID 86648749—
SolventDichloromethaneHCID 6344—
ProductMethyl cis(+/-)-2-(acetylamino)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoateHCID 86648750—

Reaction Steps

Methyl cis(±)-2-amino-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)benzoate obtained in Example (185b) (300 mg) was dissolved in methylene chloride (25 ml). Acetyl chloride (0.1 ml) and triethylamine (0.2 ml) were added, and the mixture was stirred at room temperature for one hour. Methanol was added to the reaction solution, followed by concentration under reduced pressure. Then, the residue was diluted with ethyl acetate, washed with water, and then concentrated under reduced pressure to obtain the title compound. The resulting compound was used for the next reaction without purification.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08536197B2
Source datasetuspto-grants-2013_09
ORD IDord-301e85e79ab048d3a4a677f624879237
Source noteuspto-grants-2013_09