201609-29-2

Upstream product

• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 578-57-4 2-bromoanisole 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 138647-49-1 4-Trifluoromethanesulfonyloxy-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 
• 201609-28-1 1-t-Butoxycarbonyl-4-hydroxy-4-(2-methoxyphenyl)piperidine 
• 118811-07-7 tert-butyl 4-(tosyloxy)piperidin-1-carboxylate 
• 194669-41-5 1-t-Butoxycarbonyl-4-(2-methoxyphenyl)-1,2,3,6-tetrahydropyridine 
• 5720-06-9 2-Methoxyphenylboronic acid 

Downstream Products

• 58333-75-8 4-(2-methoxyphenyl)piperidine 
• 252919-66-7 4-(2-methoxy-phenyl)-piperidine trifluoroacetate 
• 1276045-14-7 cyclopropyl-[4-(2-methoxy-phenyl)-piperidin-1-yl]-methanone 
• 1616294-18-8 2-cyclopropyl-6,7-dimethoxy-4-[4-(2-methoxy-phenyl)-piperidin-1-yl]-quinazoline 
• 82212-04-2 1,2,3,4,5,6-hexahydro-4-(2-methoxyphenyl)pyridine hydrochloride 
• 161609-76-3 4-(2-hydroxyphenyl)-piperidine 

Relevant academic research and scientific papers

2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS

Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.

Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators

Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553), a potent and brain penetrant NTR1 allosteric modulator.

Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character

The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.

Engaging nonaromatic, heterocyclic tosylates in reductive cross-coupling with aryl and heteroaryl bromides

A method has been developed for the introduction of nonaromatic heterocyclic structures onto aryl and heteroaryl bromides using alkyl tosylates in a reductive cross-coupling manifold. This protocol offers an improvement over previous methods by utilizing alkyl tosylate coupling partners that are bench-stable, crystalline solids that can be prepared from inexpensive, commercially available alcohols.

AROMATIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS

Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.

Reductive cross-coupling of nonaromatic, heterocyclic bromides with aryl and heteroaryl bromides

Reductive cross-coupling allows the direct C-C bond formation between two organic halides without the need for preformation of an organometallic reagent. A method has been developed for the reductive cross-coupling of nonaromatic, heterocyclic bromides with aryl or heteroaryl bromides. The developed conditions use an air-stable Ni(II) source in the presence of a diamine ligand and a metal reductant to allow late-stage incorporation of saturated heterocyclic rings onto aryl halides in a functional-group tolerant manner.

SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1

Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging

The synthesis and in vitro and in vivo evaluation of a new series of 7-(phenylpiperidinyl)-1,2,4-triazolo[4,3-a]pyridines, which were conveniently radiolabeled with carbon-11, as potential positron emission tomography (PET) radiotracers for in vivo imagin

Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl- cyclopropane carboxamide derivatives as novel melatonin receptor ligands

Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT1 and MT2 receptors are reported. Compounds 11f and 18b (MT 1/MT2 agonist) have human microsomal intrinsic clearance comparable to ramelteon.

Tetrahydrobenzindole compounds

A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR5; each of B and Z is independently N, CH or CR1, with the proviso that A is N when B and/or Z is N; R1, R2, R3, R4and R5and n are as defined in the specification.