7677-96-5

Upstream product

• 120-80-9 benzene-1,2-diol 
• 29976-53-2 N-ethoxycarbonyl-4-piperidone 
• 76360-25-3 1-(4,4-dimethoxypiperidin-1-yl)ethan-1-one 
• 32161-06-1 1-acetyl-4-piperidinone 
• 185316-84-1 1-(spiro[1,3-benzodioxole-2,4’-piperidine]-1-yl)ethan-1one 
• 923030-93-7 1'-(ethoxycarbonyl)spiro<1,3-benzodioxole-2,4'-piperidine> 

Downstream Products

• 1027492-97-2 (2-amino-4-(((spiro-benzo[1,3-d]-dioxol-2-yl)-piperidin-1-yl)methyl)-thiophen-3-yl)(4-chlorophenyl)methanone 
• 1456735-34-4 2-[3-(4-chlorobenzoyl)-4-(spiro-benzo[1,3-d]-dioxol-2-yl)-piperidin-1-ylmethyl-thiophen-2-yl]-isoindole-1,3-dione 
• 1456734-95-4 2-[5-bromo-3-(4-chlorobenzoyl)-4-(spiro-benzo[1,3-d]-dioxol-2-yl)-piperidin-1-ylmethyl-thiophen-2-yl]-isoindole-1,3-dione 

Relevant academic research and scientific papers

Novel tricyclic spiropiperidines. Synthesis and adrenergic activity of spiro[1,3-benzodioxolopiperidines] and spiro[1,3-benzodioxanepiperidines]

The synthesis of new series of spiropiperidines is reported. Some of these compounds showed interesting adrenergic activity. The biological activities of the new compounds were evaluated on-guinea pig atria (pi), guinea-pig trachea (β2) and rat vas deferens (a). Compounds 6a, 6c and 6f showed activity comparable to propranolol, in spite of being tertiary amines.

Synthesis of 5-oxyquinoline derivatives for reversal of multidrug resistance

The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied multidrug efflux pumps. Twelve 5-oxyisoquinoline derivatives, which are analogues of zosuquidar wherein the dibenzosuberyl-piperazine moiety is replaced by either a diarylaminopiperidine or a piperidone-derived acetal or thioacetal group, have been synthesized as pure enantiomers. Their inhibitory power has been evaluated for the bacterial multidrugresistance ABC transporter LmrCD and fungal Pdr5. Four of the newly synthesized compounds reduced the transport activity to a higher degree than zosuquidar, being up to fourfold more efficient than the lead compound in the case of LmrCD and about two times better for Pdr5.

Piperidine derivatives having anxiolytic effect

Piperidine compounds having the general formula (I), STR1 wherein R 1 is a group having general formula (II), STR2 wherein X is CHR 10, O, S, SO, SO 2 or NR 10, Z 1 is CH 2, O, or S; Z 2 and Z 3 are independently (CH 2) n, n being 0 or 1, O or S or Z 1 and Z 2 may together represent a group --CH CH--; or when Z 3 is (CH 2) n wherein n is 0, Z 1 and Z 2 may together represent a 3-membered divalent group; show potent sigma receptor activity. Furthermore they show effect in animal models indicative of anxiolytic properties. Accordingly they are useful as medicines for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases, senile demential of the Alzheimer type or Parkinson''s disease.

σ Ligands with subnanomolar affinity and preference for the σ2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines

Spiro[isobenzofuran-1(3H),4'-piperidines] and the corresponding benzofuran and benzopyran derivatives have been synthesized and evaluated as σ ligands. The compounds are related to Lu 28-179 (1'[4-[1(4fluorophenyl)-1H-indol-3- yl]-1-butyl]spiro[isobenzofu