89652-37-9

Upstream product

• 142332-70-5 3-(3,4-dimethylphenyl)propylamine 
• 306-08-1 Homovanillic acid 

Downstream Products

• 183070-49-7 2-(4-Hydroxy-3-methoxy-phenyl)-N-(3H-inden-1-ylmethyl)-acetamide 
• 96254-98-7 3-(3-{[2-(3,4-Dimethoxy-phenyl)-ethyl]-methyl-amino}-propyl)-7-hydroxy-8-methoxy-1,3,4,5-tetrahydro-benzo[d]azepin-2-one 
• 142333-36-6 KR-25003 
• 81438-44-0 7-Hydroxy-6-methoxy-1,2-diphenyl-1,4-dihydro-2H-isoquinolin-3-one 
• 81438-45-1 7-Hydroxy-6-methoxy-2-methyl-1-phenyl-1,4-dihydro-2H-isoquinolin-3-one 
• 16135-53-8 6,7-dimethoxy-1-phenyl-2-methyl-1,4-dihydro-3(2H)-isoquinolinone 
• 59443-67-3 6,7-dimethoxy-1,2-diphenyl-1,4-dihydro-2H-isoquinolin-3-one 
• 55102-37-9 (+/-)-1,2,3,4-tetrahydro-1-(4'-hydroxy-3'-methoxybenzyl)-6-methoxyisoquinolin-7-ol 
• 856259-58-0 4-(2-benzyl-7-benzyloxy-6-methoxy-1,2,3,4-tetrahydro-isoquinolin-1-ylmethyl)-2-methoxy-phenol 
• 856259-06-8 N-benzyl-N-[2-(4-benzyloxy-3-methoxy-phenyl)-ethyl]-2-(4-hydroxy-3-methoxy-phenyl)-acetamide 

Relevant academic research and scientific papers

Substituted Isoquinolinones and Quinazolinones

The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.

CATALYTIC HYDROGENATION OF NITRILES TO PRODUCE CAPSAICINOID DERIVATIVES AND AMINE COMPOUNDS, AND METHODS FOR PURIFIYING AND OBTAINING THE POLYMORPHS THEREOF

Processes for preparing an amine compound by catalytically hydrogenating a precursor nitrile compound. In a particular aspect, the present hydrogenation process occurs in a dipolar organic solvent in the presence of a palladium/carbon catalyst and a strong anhydrous protic acid. In a further aspect, the preferred embodiment relates to a process for deprotecting a compound to produce an amine compound. In yet a further aspect, the preferred embodiment relates to amine products produced by the present processes. These amine products may be used for a variety of purposes.

Anti-HIV benzylisoquinoline alkaloids and flavonoids from the leaves of Nelumbo nucifera, and structure-activity correlations with related alkaloids

(+)-1(R)-Coclaurine (1) and (-)-1(S)-norcoclaurine (3), together with quercetin 3-O-β-d-glucuronide (4), were isolated from the leaves of Nelumbo nucifera (Nymphaceae), and identified as anti-HIV principles. These compounds can serve as new leads for furt

Design, Synthesis, and Biological Evaluation of New 8-Heterocyclic Xanthine Derivatives as Highly Potent and Selective Human A2B Adenosine Receptor Antagonists

Here we report the synthesis of 8-heterocycle-substituted xanthines as potent and selective A2B adenosine receptor antagonists. The structure-activity relationships (SAR) of the xanthines synthesized in binding to recombinant human A2B adenosine receptors (ARs) in HEK-293 cells (HEK-A2B) and at other AR subtypes were explored. The synthesized compounds showed A2B adenosine receptor affinity in the nanomolar range and good levels of selectivity evaluated in radioligand binding assays at human (h) A1, A2A, A2B, and A3 ARs. We introduced several heterocycles, such as pyrazole, isoxazole, pyridine, and pyridazine, at the 8-position of the xanthine nucleus and we have also investigated different spacers (substituted acetamide, oxyacetamide, and urea moieties) on the heterocycle introduced. Various groups at the 3- and 4-positions of phenylacetamide moiety were studied. This study allowed us to identify the derivatives 2-(3,4-dimethoxyphenyl)-N-[5-(2,6-dioxo-1,3-dipropyl-2,3,6, 7-tetrahydro-1H-purin8-yl)-1-methyl-1H-pyrazol-3-yl] acetamide (29b, MRE2028F20) [Ki(hA2B) = 38 nM, Ki(hA1,hA 2A,-hA3) >1000 nM], N-benzo[1,3]dioxol-5-yl-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6, 7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy] acetamide (62b, MRE2029F20) [Ki(hA2B) = 5.5 nM, Ki(hA 1,hA2A,hA3) > 1000 nM], and N-(3,4-dimethoxyphenyl)-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6, 7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy] acetamide (72b, MRE2030F20) [Ki(hA2B = 12 nM, Ki(hA 1,hA2A, hA3) > 1000 nM], which showed high affinity at the A2B receptor subtype and very good selectivity vs the other ARs. Substitution of the acetamide with an urea moiety afforded bioisosteric xanthines with good affinity and selectivity comparable to the acetamide derivatives. Substitution at the para-position of a 4-benzyloxy group of the phenylacetamido chain enhanced affinity at the A2B receptor [compound 30b (Ki(hA2B) = 13 nM) vs compound 21b (K i(hA2B = 56 nM)] but did not favor selectivity. The derivatives with higher affinity at human A2B AR proved to be antagonists, in the cyclic AMP assay, capable of inhibiting the stimulatory effect of NECA (100 nM) with IC50 values in the nanomolar range, a trend similar to that observed in the binding assay (62b, IC50 = 38 nM; 72b, IC50 = 46 nM). In conclusion, the 8-pyrazolo-1,3-dipropyl-1H-purine-2,6-dione derivatives described herein represent a new family of selective antagonists for the adenosine A 2B receptor.

Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a new class of compounds exerting antiischemic properties

Structural modification of the calcium-antagonist verapamil (1) by replacement of the lipophilic α-isopropylacetonitrile moiety by various heterocyclic ring systems has led to a new class of cardiovascular compounds which are characterized by a specific bradycardic activity. These agents reduce heart rate without binding to classical calcium channels or β-adrenoceptors, interacting instead specifically with structures at the sino atrial node. Therefore they have also been termed sinus node inhibition. The prototype falipamil (2) has been submitted to furthr optimization mainly hy manipulation of the phthalimidine moiety. This has resultd in a secod generation of specific bradycardic agents with increased potency and selectively and prolonged duration of action represented by the benzazepinone-derivative UL-FS 49 (4). Structure-activity relationships within this novel class of compounds have revealed a marked dependence of activity on the substitution pattern of the aromatic rings, the nature of the central nitrogen atom, and the length of the connecting alkyl chains. The crucial role of the benzazepione ring for bradycardic activity can be best explained by its special impact on the overall molecular conformation.