87109-89-5

Upstream product

• 59234-46-7 dimethyl (2R,6S)-piperidine-2,6-dicarboxylate 
• 100-39-0 benzyl bromide 
• 111-16-0 heptanedioic acid 
• 142-79-0 pimeloyl chloride 
• 5453-67-8 2,6-bis(methoxycarbonyl)pyridine 
• 499-83-2 Pyridine-2,6-dicarboxylic acid 
• 408320-48-9 2,6-Dibromo-heptanedioyl dichloride 
• 868-73-5 dimethyl 2,6-dibromoheptadioate 
• 100-46-9 benzylamine 

Downstream Products

• 246245-91-0 (2R,6R)-1-(phenylmethyl)-2-(2-propen-1-yl)-2,6-piperidinedicarboxylic acid dimethyl ester 
• 246031-44-7 (2R,6R)-1,2-Dibenzyl-piperidine-2,6-dicarboxylic acid dimethyl ester 
• 130291-44-0 (2S,6S)-1-Benzyl-2,6-bis-benzyloxymethyl-piperidine 

Relevant academic research and scientific papers

CONJUGATES OF 2,4-ETHANO-BRIDGED AND 2,4-PROPANO-BRIDGED 3,6,9-TRIAZA-NONANOIC ACID, 3N,6N,9,9N-TETRAETHANOIC ACID, AND CORRESPONDING PHOSPHORIC ACID METHYLENE DERIVATIVES AND THE SUBSTITUTION PRODUCTS THEREOF WITH BIOMOLECULES, METHODS FOR THE PRODUCTION THEREOF, AND THE USE OF THE SAME FOR PRODU

The invention relates to conjugates of 2,4-ethano-bridged and 2,4-propano-bridged 3,6,9-triaza-nonanoic acid, N,N,N-tetraethanoic acid, and corresponding phosphoric acid ester methylene derivatives of formula (1) - wherein the substituents are defined as cited in patent claim 1 - and the substitution products thereof with biomolecules. The invention also relates to methods for producing said conjugates and to the use of the same as contrasting media in NMR diagnosis and radiodiagnosis, and for radiotherapy.

Synthesis of DTPA analogues derived from piperidine and azepane: Potential contrast enhancement agents for magnetic resonance imaging

Two DTPA derivatives (PIP-DTPA and AZEP-DTPA) as potential contrast enhancement agents in MRI are synthesized. The T1 and T2 relaxivities of their corresponding Gd(III) complexes are reported. At clinically relevant field strengths, the relaxivities of the complexes are comparable to that of the contrast agent, Gd(DTPA) which is in clinical use. The serum stability of the 153Gd-labeled complexes is assessed by measuring the release of 153Gd from the ligands. The radiolabeled Gd chelates are found to be kinetically stable in human serum for up to at least 14 days without any measurable loss of radioactivity.

Synthesis, modelling, and μ-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes

A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropenyl isomers (2a-g), as homologues of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (I-II), were synthesized and evaluated for the binding affinity towards opioid receptor subtypes μ, δ and κ. Compounds 1a-g and 2a-g exhibited a strong selective μ-affinity with Ki values in the nanomolar range, which favourably compared with those of I and II. In addition, contrary to the trend observed for DBO-I, II, the μ-affinity of series 2 is markedly higher than that of the isomeric series 1. This aspect was discussed on the basis of the conformational studies performed on DBN which allowed hypotheses on the mode of interaction of these compounds with the μ receptor.

Highly enantioselective synthesis of substituted piperidines using the chiral lithium amide base approach

The symmetry-breaking enolisation reaction of a meso-piperidine diester using a chiral bis-lithium amide base allows access to alkylated derivatives in highly diastereo- and enantioselective fashion (> 98% ee).