150986-62-2

Usage

Uses

Used in Organic Synthesis:
N-BOC-(3R,4R)-3,4-PYRROLIDINEDIOL is used as a reagent in organic synthesis for its ability to facilitate specific chemical reactions due to its stereochemistry and protecting group. N-BOC-(3R,4R)-3,4-PYRROLIDINEDIOL aids in the formation of complex organic molecules by enabling selective functionalization.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, N-BOC-(3R,4R)-3,4-PYRROLIDINEDIOL is used as a building block for the preparation of various pharmaceuticals and natural products. Its stereochemical purity and reactivity make it an essential component in the synthesis of bioactive compounds and drug candidates.
Used in Natural Product Synthesis:
N-BOC-(3R,4R)-3,4-PYRROLIDINEDIOL is also utilized in the synthesis of natural products, where its specific stereochemistry and reactivity are crucial for replicating the complex structures found in nature. This application is vital for the development of new drugs and therapeutic agents derived from natural sources.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 90481-32-6 (3S,4S)-pyrrolidine-3,4-diol 
• 90365-74-5 (3S,4S)-(+)-1-benzyl-3,4-pyrrolidinediol 
• 1428671-12-8 (3S,4S)-1-(tert-butoxycarbonyl)-3,4-pyrrolidinediyl diacetate 
• 163439-82-5 (3R,4R)-1-benzyl-3,4-pyrrolidinediol 
• 186393-31-7 (3R,4R)-pyrrolidine-3,4-diol 
• 114214-49-2 1-tert-butoxycarbonyl-3,4-epoxypyrrolidine 
• 762-75-4 tert-butyl formate 

Downstream Products

• 722545-09-7 (+)-(3R,4R)-1-tert-butoxycarbonyl-3,4-bis(phenylsulfanyl)pyrrolidine 
• 926913-07-7 (3S,4S)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)-4-hydroxypyrrolidine 
• 557-40-4 Allyl ether 
• 1374429-77-2 (3R,4S)-tert-butyl 3-azido-4-(bis(4-methoxyphenyl)(phenyl)methoxy)pyrrolidine-1-carboxylate 
• 1412256-91-7 (3R,4S)-tert-butyl 3-(benzyloxycarbonylamino)-4-(bis(4-methoxyphenyl)(phenyl)methoxy)pyrrolidine-1-carboxylate 
• 1193318-61-4 (3S,4R)-4-amino-1-N-Boc-3-dimethoxytrityloxypyrrolidine 
• 372482-11-6 tert-butyl (3S,4S)-3-hydroxy-4-methoxypyrrolidine-1-carboxylate 
• 694439-03-7 tert-butyl (4aS,7aS)-hexahydro-6H-[1,4]dioxino[2,3-c]pyrrolidine-6-carboxylate 
• 926912-89-2 (3R,4R)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)-4-hydroxypyrrolidine 
• 148214-86-2 tert-butyl (3R,4R)-3-hydroxy-4-methoxypyrrolidine-1-carboxylate 
• 926913-03-3 (3R,4R)-4-(adenin-9-yl)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)pyrrolidine 
• 926912-93-8 (3R,4S)-4-(adenin-9-yl)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)pyrrolidine 
• 926913-01-1 (3R,4R)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)-4-(thymin-1-yl)-pyrrolidine 
• 926912-92-7 (3R,4S)-1-N-tert-butyloxycarbonyl-3-(4,4'-dimethoxytrityloxy)-4-(thymin-1-yl)-pyrrolidine 

Relevant academic research and scientific papers

Selective Isomerization via Transient Thermodynamic Control: Dynamic Epimerization of trans to cis Diols

Traditional approaches to stereoselective synthesis require high levels of enantio- and diastereocontrol in every step that forms a new stereocenter. Here, we report an alternative approach, in which the stereochemistry of organic substrates is selectivel

Compound JK-03M having higher protein kinase G inhibitory activity or pharmaceutically acceptable salt thereof and preparation method thereof

The invention discloses a compound which has higher protein kinase G inhibitory activity and is shown in a formula I or pharmaceutically acceptable salt thereof and a preparation method thereof. The compound JK-03M having the higher protein kinase G inhibitory activity comprises a pharmaceutical composition of a new compound and application of the new compound in treatment of pain, in particular to chronic pain. The formula (1) is shown in the description.

Compounds with higher PKG (protein kinase G) inhibitory activity and preparation method of compounds

The invention discloses compounds which have higher PKG (protein kinase G) inhibitory activity and are represented as a formula I, pharmaceutically acceptable salts, pharmaceutical composition containing the novel compounds, as well as an application of the novel compounds in treatment of pain, especially chronic pain. The invention further discloses a preparation method of the compounds and new intermediates. R1 and R2 are the same or different and are selected from a group comprising halogen (such as F or Cl), C1-C6 alkoxy, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl; R3 is a terminal group and is selected from a group comprising H, halogen, alkyl, naphthenic base, alkenyl, alkynyl, aryl and heteroaryl; n is the number of repetitive units and is an integer in a range from 1 to 15.

COMPOUND HAVING HIGHER INHIBITION OF PROTEIN KINASE G ACTIVITY AND PREPARATION METHOD THEREFOR

Disclosed are a compound of Formula I having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R1 and R2 are the same or different, each being independently chosen from the halogens, the C1-C6 alkoxyl group, the C1-C6 alkyl group, the C2-C6 alkenyl group, and the C2-C6 alkynyl group; R3 is chosen from H, the halogens, the substituted or unsubstituted C1-C6 alkyl group, C3-C6 cycloalkyl group, C2-C6 alkenyl group, and C2-C6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.

PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyrazolo[1,5-a]pyrimidine-5,7- diamine compounds (referred to herein as "PPDA compounds") that, inter alia, inhibit (e.g., selectively inhibit) CDK (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CDK; and to treat disorders including: disorders that are associated with CDK; disorders that result from an inappropriate activity of a cyclin-dependent kinase (CDK); disorders that are associated with CDK mutation; disorders that are associated with CDK overexpression; disorders that are associated with upstream pathway activation of CDK; disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischaemia; renal diseases; and cardiovascular disorders (including atherosclerosis). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with a further active agent which is, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

HETEROCYCLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY

The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a

A broadly applicable and practical oligomeric (salen)Co catalyst for enantioselective epoxide ring-opening reactions

The (salen)Co catalyst (4a) can be prepared as a mixture of cyclic oligomers in a short, chromatography-free synthesis from inexpensive, commercially available precursors. This catalyst displays remarkable enhancements in reactivity and enantioselectivity relative to monomeric and other multimeric (salen)Co catalysts in a wide variety of enantioselective epoxide ring-opening reactions. The application of catalyst 4a is illustrated in the kinetic resolution of terminal epoxides by nucleophilic ring-opening with water, phenols, and primary alcohols; the desymmetrization of meso epoxides by addition of water and carbamates; and the desymmetrization of oxetanes by intramolecular ring opening with alcohols and phenols. The favorable solubility properties of complex 4a under the catalytic conditions facilitated mechanistic studies, allowing elucidation of the basis for the beneficial effect of oligomerization. Finally, a catalyst selection guide is provided to delineate the specific advantages of oligomeric catalyst 4a relative to (salen)Co monomer 1 for each reaction class.

Five-membered iminocyclitol α-glucosidase inhibitors: Synthetic, biological screening and in silico studies

The design and synthesis of a small library of pyrrolidine iminocyclitol inhibitors with a structural similarity to 1,4-dideoxy-1,4-imino-d-arabitol (DAB-1) is reported. This library was specifically designed to gain a better insight into the mechanism of inhibition of glycosidases by polyhydroxylated pyrrolidines or iminocyclitols. Pyrrolidine-3,4-diol 15a and pyrrolidine-3,4-diol diacetate 15b had emerged as the most potent α-glucosidase inhibitors in the series. Docking studies performed with an homology model of α-glucosidase disclosed binding poses for compounds 15a, 15b, 16a, and 16a′ occupying the same region as the NH group of the terminal ring of acarbose and suggest a closer and stronger binding of compound 15a and 15b with the enzyme active site residues. Our studies indicate that 2 or 5-hydroxyl substituents appear to be vital for high inhibitory activity.

TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS

Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.

Low-generation dendrimers with a calixarene core and based on a chiral C2-symmetric pyrrolidine as iminosugar mimics

The preparation of low-generation dendrimers based on a simple calix[4]arene scaffold by insertion of the iminosugar-analogue C 2-symmetric 3, 4-dihydroxypyrrolidine is described. This methodology allows a rapid incorporation of a considerable number of iminosugar-like moieties in a reduced volume and in a well-defined geometry. The inclusion of alkali-metal ions (sodium and potassium) in the polar cavity defined by the acetamide moieties at the lower rim of the calixarene was demonstrated, which allows also the rigidification of the dendrimer structure and the iminosugar presentation in the clusters. The combination of the supra-molecular properties of calixarenes with the advantage of a dendrimeric presentation of repetitive units opens up the possibility of generating well-defined multivalent and multifaceted systems with more complex and/or biologically relevant iminosugars.