Hydrochloric Acid → (S)-N1-(2-amino-ethyl)-N4-[(S)-1-(amino-imino-methyl)-piperidin-3-ylmethyl]-N1-cyclopropyl-2-morpholin-4-ylsulphonylamino-succinamide hydrochloride

Participants

Reaction Steps

2.77 g of benzyl 2-[[(S)-3-[(S)-1-(amino-imino-methyl)-piperidin-3-ylmethyl-carbamoyl]-2-morpholin-4-ylsulphonylamino-propionyl]-cyclopropyl-amino]-ethylcarbamate (Example 23) are dissolved in 90 ml of methanol. After the addition of 2.13 ml of 2N hydrochloric acid and 300 mg of Pd/C (10%) the mixture is hydrogenated at room temperature for 1.5 hours, the catalyst is then filtered off and the filtrate is evaporated. The residue is dispersed with ether and the white crystals are filtered off. 2.44 g of crystalline (S)-N1-(2-amino-ethyl)-N4-[(S)-1-(amino-imino-methyl)-piperidin-3-ylmethyl]-N1-cyclopropyl-2-morpholin-4-ylsulphonylamino-succinamide hydrochloride (1:2), MS (ISP): 503.4 (M+H), are obtained.

Provenance & Evidence