88790-38-9

Usage

Uses

Used in Pharmaceutical Research:
(S)-1-Boc-2-(2-hydroxyethyl)pyrrolidine is used as a building block for the synthesis of various bioactive compounds, contributing to the development of new medicinal agents and potential drug candidates. Its versatile reactivity and chiral nature make it a valuable component in the creation of innovative pharmaceuticals.
Used in Organic Synthesis:
In the field of organic synthesis, (S)-1-Boc-2-(2-hydroxyethyl)pyrrolidine is employed as a reagent, facilitating the construction of complex molecular structures. Its unique properties, including the Boc protecting group, allow for selective reactions and the formation of diverse chemical entities.
Used in Medicinal Chemistry:
(S)-1-Boc-2-(2-hydroxyethyl)pyrrolidine is utilized as a key intermediate in the synthesis of pharmaceutically relevant compounds, enabling the exploration of novel therapeutic agents with improved efficacy and selectivity. Its chiral center and functional groups provide opportunities for the design of enantioselective catalysts and ligands, further enhancing the scope of medicinal chemistry research.

Upstream product

• 56502-01-3 (2S)-1-tert-butoxycarbonyl-2-carboxymethylpyrrolidine 
• 34619-03-9 tert-butyldicarbonate 
• 543-27-1 isobutyl chloroformate 
• 115393-77-6 tert-butyl (S)-2-vinylpyrrolidine-1-carboxylate 
• 69610-41-9 Boc-L-Pro-H 
• 59936-29-7 (S)-N-(tert-butoxycarbonyl)proline methyl ester 
• 69610-40-8 N-(tert-butoxycarbonyl)-L-prolinol 
• 646062-88-6 (E)-(6-tert-butoxycarbonylamino)-2-hexenal 
• 198493-30-0 tert-butyl (2S)-2-(2-oxoethyl)pyrrolidine-1-carboxylate 
• 147-85-3 L-proline 
• 101130-03-4 tert-butyl (S)-2-(diazoacetyl)pyrrolidine-1-carboxylate 
• 141874-26-2 N-Boc-(S)-proline chloride 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 84890-94-8 (S)-2-Isobutoxycarbonyloxycarbonyl-pyrrolidine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 1433607-48-7 (E)-2-amino-7-(4-fluoro-2-(pyridin-3-yl)phenyl)-4-methyl-7,8-dihydro-6H-quinazolin-5-one O-((S)-2-(pyrrolidin-2-yl)ethyl)oxime 
• 1433607-57-8 (2S)-N-Boc-2-(((2-((E)-2-amino-7-(4-fluoro-2-(pyridin-3-yl)phenyl)-4-methyl-7,8-dihydro-6H-quinazolin-5-ylidene)amino)oxy)ethyl)pyrrolidine 
• 933746-73-7 (S)-2-(2-methoxyethyl)pyrrolidine 
• 1334123-13-5 C₂₃H₃₃FN₂O₃ 
• 937203-20-8 (S)-N-Boc-2-(bromoethyl)pyrrolidine 
• 191528-61-7 Carbonic acid 2-[(S)-1-(2-azido-benzoyl)-pyrrolidin-2-yl]-ethyl ester methyl ester 
• 191528-62-8 (2-Azido-phenyl)-[(S)-2-(2-hydroxy-ethyl)-pyrrolidin-1-yl]-methanone 
• 191528-63-9 [(S)-1-(2-Azido-benzoyl)-pyrrolidin-2-yl]-acetaldehyde 
• 335203-32-2 (3S,7S)-1-aza-3-benzyl-3-methyl-4-thiabicyclo[5.3.0]-2-decanone 
• 335203-33-3 3-R-7-S-1-aza-3-benzyl-3-methyl-4-thiabicyclo[5.3.0]-2-decanone 

Relevant academic research and scientific papers

Tetrahydropyrido [3, 4-d] pyrimidine derivative and medical application thereof

The invention relates to a compound as shown in a general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate and a preparation method thereof, and application of the compound in preparation of drugs for treating diseases related to KRas-G12C activity or expression quantity.

PYRIDAZINONES AS PARP7 INHIBITORS

The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects

Currently used antipsychotics are characterized by multireceptor mode of action. While antagonism of dopamine D2 receptors is responsible for the alleviation of “positive” symptoms of schizophrenia and the effects at other, particularly serotonergic receptors are necessary for their additional therapeutic effects, there is no consensus regarding an “ideal” target engagement. Here, a detailed SAR analysis in a series of 45 novel azinesulfonamides of cyclic amine derivatives, involving the aryl-piperazine/piperidine pharmacophore, central alicyclic amine and azinesulfonamide groups has led to the selection of (S)-4-((2-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)isoquinoline (62). The polypharmacology profile of 62, characterized by partial 5-HT1AR agonism, 5-HT2A/5-HT7/D2/D3R antagonism, and blockade of SERT, reduced the “positive”-like, and “negative”-like symptoms of psychoses. Compound 62 produced no catalepsy, demonstrated a low hyperprolactinemia liability and displayed pro-cognitive effects in the novel object recognition task and attentional set-shifting test. While association of in vitro features with the promising in vivo profile of 62 is still not fully established, its clinical efficacy should be verified in further stages of development.

(QUINOLINE OR ISOQUINOLINE)SULFONAMIDES OF CYCLIC AMINES AS ANTIPSYCHOTIC DRUGS

The invention relates to compounds of general formula (I) wherein: one of A1 and A2 represents a nitrogen atom and the other a carbon atom optionally substituted by halogen; the wave line between the sulfonamido moiety and B/C rings represents a single bond linking the sulfur atom to a non-bridgehead carbon atom, with the proviso that the part of ring C being detached by the dashed broken line is unsubstituted; n represents an integer from 0 to 3; Y represents a nitrogen or carbon atom; Z represents a 5-6 membered aromatic/ heteroaromatic ring optionally fused with a further aromatic or non- aromatic 5-6 membered heterocycle, the condensed ring system being linked via a non-bridgehead carbon atom. The compounds display high affinity for the D2, D3, 5-HT1A, 5-HT2A- 5-HT6 and 5-HT7 receptors and are useful for the treatment of psychotropic diseases or disorders associated with disturbances of the dopaminergic/ serotoninergic systems such as schizophrenia and autism.

IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS

The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.

IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS

The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.

AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES

The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

SUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINES AS MKNK1 INHIBITORS

The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): (Ia) (Ib) (Ic) (Id) in which A, Y, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

QUINAZOLINE DERIVATIVES WITH HSP90 INHIBITORY ACTIVITY

Compounds of general formula (I): or a stereoisomer, tautomer, polymorph, hydrate, solvate, or a pharmaceutically acceptable salt thereof, wherein R is as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as proliferative diseases, e.g. cancers, viral and fungal infections, neurodegenerative or inflammatory diseases or conditions. The invention also relates to the preparation of these compounds as well as to pharmaceutical compositions comprising them.

Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: Nonradioactive counterparts of putative PET-compatible apoptosis imaging agents

Downstream caspases-3 and -7 are essential to execute the programmed type I cell death (apoptosis). In order to better understand their role, specific inhibitors of these enzymes are required, which after radiolabeling can be applied to non-invasively visualize and monitor apoptotic pathways in vivo using Positron Emission Tomography (PET). Therefore, 2-methoxyethyl-, 2-methoxypropyl-, 2-ethoxymethyl-, 2-(2-fluoroethoxymethyl)-, and 2-(2,2,2-trifluoroethoxymethyl)pyrrolidinyl analogues of (S)-5-[1-(2- methoxymethylpyrrolidinyl)sulfonyl]isatin (2) were prepared and their in vitro binding affinities towards caspases-1, -3, -6 and -7 were evaluated and compared to that of the lead structure 2. While the inhibition potencies against caspases-1 and -6 were in the micromolar range, all synthesized compounds exhibited excellent and selective inhibition of caspases-3 and -7 in the nanomolar range up to IC50 = 4.79 nM and 7.47 nM, respectively. These highly potent 2-substituted analogues of 2 might be developed as anti-apoptosis agents and some selected fluorinated inhibitors might be useful as potential PET radiotracers for apoptosis imaging after 18F-labeling.