167710-67-0

Upstream product

• 3612-20-2 1-phenylmethyl-4-piperidone 
• 97-62-1 Ethyl isobutyrate 
• 600-00-0 ethyl 2-bromoisobutyrate 

Downstream Products

• 478363-91-6 1,2,3,6-tetrahydro-α,α-dimethyl-1-phenylmethyl-4-piperidineacetic acid ethyl ester 
• 167781-58-0 1-dodecyl-N-methyl-N-phenylmethyl-α,α-dimethyl-4-piperidineacetamide 

Relevant academic research and scientific papers

Preparation method of piperidine spiro derivative

The invention discloses a preparation method of a piperidine spiro derivative, and belongs to the field of synthesis of medical intermediates. The method comprises the following steps: 1, enabling N-benzyl substituted cyclic ketone 1 to react with bromo-c

SPIROCYCLIC COMPOUNDS AS AGONISTS OF THE MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR

This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula. (I) where p, q, r, s, X, Z, Y, R1, R2, R3and R4 are as defined herein.

MUSCARINIC RECEPTOR AGONISTS

This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.

DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS

Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Structure activity relationships of new inhibitors of mammalian 2,3-oxidosqualene cyclase designed from isoquinoline derivatives

We have designed more potent inhibitors from the previously reported LF 05-0038, a 6-isoquinolinol based inhibitor of 2,3-oxidosqualene cyclase (IC 50: 1.1 μM). Replacement of the 3-OH group by various 3-substituted amino groups, and modification of the alkyl chain borne by the endocyclic nitrogen led to inhibitors with IC50 in the range of 0.15 to 1 μM. In a second step, opening of the bicyclic ring system afforded the corresponding aminoalkylpiperidines which were slightly more potent. Finally, introduction of suitable aromatic containing moieties on the piperidine nitrogen yielded very potent inhibitors such as 20x (IC50=18 nM) easy to synthesize and achiral. The recent availability of the crystal structure of squalene-hopene cyclase allowed us to construct a three-dimensional (3D) model of the related 2,3-oxidosqualene cyclase (OSC) which was tentatively used to describe the possible mode of binding of our compounds and which can be useful for designing new inhibitors.

Preparation of 4-(2-aminoethyl)-3,3-dimethyl-2-piperidone derivatives by intramolecular rearrangement of α,α-dimethyl-4-piperidineacetyl chloride

Reaction of hindered amines with α,α-dimethyl-4-piperidineacetyl chloride provided 4-(2-aminoethyl)-3,3-dimethyl-2-piperidone derivatives by intramolecular rearrangement of the acid chloride.