203186-96-3

Usage

Uses

Used in Pharmaceutical Industry:
1-BOC-4-AMINO-PIPERIDINE-4-METHANOL is used as a chemical intermediate for the synthesis of various pharmaceutical compounds. Its BOC protecting group allows for selective deprotection to expose the amine group, which is crucial for the formation of amide bonds and other functional groups in drug molecules.
Used in Organic Synthesis:
1-BOC-4-AMINO-PIPERIDINE-4-METHANOL is used as a versatile building block in organic synthesis for the creation of complex organic molecules. The BOC protecting group enables selective reactions, while the hydroxyl group provides opportunities for further derivatization and functionalization, expanding the compound's applicability in the synthesis of diverse organic structures.
Used in Drug Discovery:
1-BOC-4-AMINO-PIPERIDINE-4-METHANOL is used as a key component in drug discovery processes. Its unique structure and functional groups make it a promising candidate for the development of new pharmaceutical agents, particularly in the areas of medicinal chemistry and drug design.

Upstream product

• 1187321-32-9 4-aminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester 
• 1187321-31-8 4-benzyloxycarbonylaminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester 
• 1093214-64-2 1-(tert-butoxycarbonyl)-4-(ethoxycarbonyl)piperidine-4-carboxylic acid 
• 183673-71-4 4-amino-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid 

Downstream Products

• 917834-41-4 tert-butyl 4-(benzyloxycarbonylamino)-4-(hydroxymethyl)piperidine-1-carboxylate 
• 1187321-35-2 (4-fluoromethylpiperidin-4-yl)carbamic acid benzyl ester 
• 1187321-34-1 tert-butyl 4-(benzyloxycarbonylamino)-4-(fluoromethyl)piperidine-1-carboxylate 

Relevant academic research and scientific papers

Discovery of 3-chlorobenzyl-linked 1,9-diazaspiro[5.5]undecane derivatives, a lead for dengue virus type 2 infection

Dengue virus poses a serious worldwide health threat with up to 400 million infections occurring annually in over 100 countries. Currently, there are no specific therapeutics available, and the only licensed vaccine is used to mitigate the risk of hospitalization in immunologically naive individuals. In the current work, for the first time we are reporting dengue virus type 2 (DENV2) inhibitory activity in newly designed 3-chlorobenzyl-linked 1,9-diazaspiro[5.5]undecane derivatives. Compounds with substitutions featuring 2-methylbenzyl (SPO-6, EC50 = 11.43 ± 0.87 μM), 4-bromobenzyl (SPO-7, EC50 = 14.15 ± 0.50 μM), and 4-cyanobenzyl (SPO-13, EC50 = 20.77 ± 1.92 μM) groups and the antiviral drug ribavirin (IC50 = 50.9 ± 18 μM, J. Gen. Virol., 2006, 87, 1947–1952) were found to be potent against DENV2 in a cell-based assay. Docking calculations identified NS5-methyltransferase as the most probable target for this series of compounds. Molecular dynamics simulations of NS5-methyltransferase reproduced the experimental binding affinity findings by yielding ΔGbind values that predicted SPO-6 to possess the most favorable binding energy of ?27.2 ± 3.9 kcal mol?1 compared with SPO-7, SPO-13 and ribavirin with ?22.5 ± 4.7, ?22.5 ± 4.6 and ?20.0 ± 4.6 kcal mol?1, respectively. In addition, based on Lipinski's rule of five, SPO-6 was found to be non-toxic and possessed a better drug-likeness score (5.87) in comparison with the standard drug ribavirin (1.72).

1,4,9-Triazaspiro[5.5]undecan-2-one Derivatives as Potent and Selective METTL3 Inhibitors

N6-methyladenosine (m6A) is the most frequent of the 160 RNA modifications reported so far. Accumulating evidence suggests that the METTL3/METTL14 protein complex, part of the m6A regulation machinery, is a key player in a variety of diseases including several types of cancer, type 2 diabetes, and viral infections. Here we report on a protein crystallography-based medicinal chemistry optimization of a METTL3 hit compound that has resulted in a 1400-fold potency improvement (IC50 of 5 nM for the lead compound 22 (UZH2) in a time-resolved F?rster resonance energy transfer (TR-FRET) assay). The series has favorable ADME properties as physicochemical characteristics were taken into account during hit optimization. UZH2 shows target engagement in cells and is able to reduce the m6A/A level of polyadenylated RNA in MOLM-13 (acute myeloid leukemia) and PC-3 (prostate cancer) cell lines.

Bespoke SnAP reagents for the synthesis of c-substituted spirocyclic and bicyclic saturated N-heterocycles

The precise placement of C-substituents on bicyclic and spirocyclic N-heterocycles is readily achieved by the combination of aldehydes and new SnAP reagents. The substituted SnAP reagents are readily prepared from simple starting materials and couple with

NOVEL DERIVATIVES OF ACYL CYANOPYRROLIDINES

A compound of formula (I) or a tautomeric form, regioisomer, stereoisomer, solvate, N-oxide or pharmaceutically acceptable salts thereof; wherein 'a' - is selected from the group consisting of substituted or unsubstituted heterocycloalkyl ring and substituted or unsubstituted carbohydrate moiety y is a member selected from -O-, -CO-, -S02-, aminoalkyl or formula (II) wherein, Rw is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; x is a member selected from -0-, -S-, -SO-, -S02-, CONR10, NR10CO and -NRd-, or x and y together represent a chemical bond; Z is selected from -CH-, -N-. t is an integer selected from O to 4; with the provisos that when 'a' is substituted or unsubstituted heterocycloalkyl ring then 't' is not O and when y = -CO-, x is not NRd.