Category: 1239319-82-4

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Safety of tert-Butyl 2-amino-7-azaspiro[3.5]nonane-7-carboxylate, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1239319-82-4, Name is tert-Butyl 2-amino-7-azaspiro[3.5]nonane-7-carboxylate, molecular formula is C13H24N2O2. In a Patent, authors is ，once mentioned of 1239319-82-4

The present invention relates to a compound of Formula (I)-(IV) useful as beta-lactamase inhibitor, a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein R1, R2, M and ring A have definitions as those in the specification. The present invention further relates to methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and uses of these compounds. For example, the compounds of the present invention can be used as beta-lactamase inhibitors, for treatment and/or prophylaxis of diseases caused by bacterial infections, solving drug-resistance problems caused by beta-lactamases, especially bacterial drug-resistant diseases caused by type B metallo-beta-lactamases.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 1239319-82-4, help many people in the next few years.Safety of tert-Butyl 2-amino-7-azaspiro[3.5]nonane-7-carboxylate

Reference：
Piperidine – Wikipedia,
Piperidine | C5H19951N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1239319-82-4,tert-Butyl 2-amino-7-azaspiro[3.5]nonane-7-carboxylate,as a common compound, the synthetic route is as follows.

1239319-82-4, A solution of the appropriate chloride (1 eq) (ex: 5-chloro-6-methyl-3-(3- trifluoromethoxy-phenyl)-7,8-dihydro-6H-9-oxa-1 ,2,3a,4,6-pentaaza-cyclopenta- (ajnaphthalene) and the appropriate amine (3 to 5 eq) (ex: 1-methyl-piperidin-4- ylamine) in nBuOH (15 mL/mmol) was heated up to 180- 185C under microwave irradiation for 5 h – 10 h (or 24 h at 160-180C in a silicon bath). The solvent was evaporated under vacuum and the residue was purified by flash chromatography (Isolute/Flash, Sill, 2.5% MeOH with 7N ammonia in DCM) or by semi-preparative HPLC (Gemini C18 (150 10 mm; 5 m), Solvent A: water with 0.1 % formic acid; Solvent B: acetonitrile with 0.1 % formic acid. Gradient: 40% of A to 0% of A).The NH-BOC-protected amines got deprotected in the reaction conditions and reacted giving a mixture of regioisomers. Amine: 2-amino-7-aza-spiro[3.5]nonane-7-carboxylic acid tert-butyl esterExample 487-[6- ethyl-3-(3-trifluoromethoxy-phenyl)-7,8-dihydro-6H-9-oxa-1 ,2,3a,4,6- pentaaza-cyclopenta[a]naphthalen-5-yl]-7-aza-spiro[3.5]non-2-ylamineHPLC-MS (method 1 ): Rt=3.37 min, [M+H]+m/z 490.2.1H NMR (700 MHz, MeOD) delta 8.49 (s, 1 H), 8.42 – 8.36 (m, 1 H), 7.66 (td, J = 8.1 , 2.2 Hz, 1 H), 7.42 (d, J = 8.2 Hz, 1 H), 4.45 – 4.39 (m, 2H), 3.47 (ddd, J = 30.1 , 20.6, 10.2 Hz, 4H), 2.96 (d, J = 4.9 Hz, 3H), 2.37 (s, 1 H), 2.34 – 2.27 (m, 2H), 1.90 (dd, J = 12.6, 7.5 Hz, 3H), 1.81 (ddd, J = 22.6, 10.9, 5.6 Hz, 4H), 1.65 (dd, J = 12.3, 8.3 Hz, 2H).Example 49(7-Aza-spiro[3.5]non-2-yl)-[6-methyl-3-(3-trifluoromethoxy-phenyl)-7,8- dihydro-6H-9-oxa-1 ,2,3a,4,6-pentaaza-cyclopenta[a]naphthalen-5-yl]-amineHPLC-MS (method 1 ): Rt=3.21 min, [M+H]+m/z 490.2.1H NMR (300 MHz, MeOD) delta 8.60 (s, 1 H), 8.37 (d, J = 8.0 Hz, 1 H), 7.66 (t, J = 8.1 Hz, 1 H), 7.44 (d, J = 8.3 Hz, 1 H), 4.56 – 4.44 (m, 2H), 4.38 (dd, J = 16.0, 8.0 Hz, 1 H), 3.28 (dd, J = 6.9, 2.5 Hz, 2H), 3.25 – 3.15 (m, 2H), 3.16 – 3.05 (m, 2H), 2.79 (s, 3H), 2.59 – 2.44 (m, 2H), 2.07 – 1.92 (m, 4H), 1.92 – 1.81 (m, 2H).

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Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); GARCIA COLLAZO, Ana Maria; PASTOR FERNANDEZ, Joaquin; BLANCO APARICIO, Carmen; RODRIGUEZ HERGUETA, Antonio; MARTIN HERNANDO, Jose Ignacio; RAMOS LIMA, Francisco Javier; HERNANDEZ HIGUERAS, Ana Isabel; SALUSTE, Carl-Gustave Pierre; GONZALEZ CANTALAPIEDRA, Esther; MARTINEZ GONZALEZ, Sonia; SALGADO SERRANO, Antonio; NOYA MARINO, Beatriz; WO2011/80510; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem