4-(2-Aminoethyl)-1-Boc-piperidine

A mixture of tert-butyl 4-(cyanomethyl)piperidine-1-carboxylate (20 g, 89.29 mmol) and NH5.5 g (15.34 mmol) of tert-butyl 4-(2-(1, 3-dioxoisoindolin-2-yl)ethyl)piperidine-1-carboxylate prepared previously are solubilized in 40 ml of ethanol amine and the mixture is stirred at room temperature for 5.5 h. To the tert-butyl 4-(2-(1, 3-dioxoisoindolin-2-yl)ethyl)piperidine-1-carboxylate (245 g) in ethanol ( 2 L) was added hydrazine hydrate (55 mL, ~1 mol) in one portion and the mixture heated to 50-60 °C for 22 hours. The resulting slurry was cooled to 30 °C, filtered and washed with ethanol (800 mL). The filtrate was evaporated, taken up in CHGeneral procedure: To a mixture of(48 mg, 0.13 mmol) in DMF (1.5 mL, HATU (69 mg, 0.18 mmol), DIPEA (45uL, 0.26 mmol) and) The 2, 4 - dichloro pyrimidine -5 - carboxamide (200 mg, 1 . 04 mmol) dissolved in tetrahydrofuran (5 ml) in, respectively adding 4 - (2 - aminoethyl) piperidine -1 - formic acid tert-butyl (238 mg, 1 . 04 mmol) and diisopropyl serotonin reuptake (404 mg, 3 . 13 mmol), 25 C reaction 2 hours. Add saturated salt water (50 ml), stirring 15 minutes after the filtering, the filter cake washing petroleum ether, to obtain white solid 270 mg, yield 68%[0474] Procedure: To a stirred solution of [0439] Procedure: To a stirred solution of

Molecular Weight:228.33
XLogP3:1.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:4
Exact Mass:228.183778013
Monoisotopic Mass:228.183778013
Topological Polar Surface Area:55.6
Heavy Atom Count:16
Complexity:228
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes