227954-87-2Relevant academic research and scientific papers
Of escitalopram oxalate-related substance and its preparation method
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Paragraph 0035; 0036, (2018/12/13)
The invention relates to an escitalopram oxalate related substance and a preparation method thereof, and particularly, relates to the related substance of an antidepressant drug, the escitalopram oxalate (namely, (S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-formonitrile oxalate), represented as the formula (I) and a preparation method thereof. The escitalopram oxalate, as the target compound, is synthesized through reactions comprising hydrolysis, acylation, condensation, reduction, addition and oxidization to the compound (II) (namely, (S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-formonitrile). According to the method, the compound (I) is chemically synthesized for the first time. By means of the method, the target compound can be obtained through high-efficient and quick separation.
Preparation method of escitalopram oxalate impurities
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Paragraph 0018, (2017/08/29)
The application of the invention provides a brand-new preparation method of (R)-4-(dimethylamino)-1-(1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-yl)-butyl-1-ketone to provide a basis for qualitative and quantitative analysis of impurity profiles in escitalopram oxalate finished products, thereby having a significant role in quality control of escitalopram oxalate and being capable of promoting the safe use of depressive patients.
Histamine-3 Receptor Antagonists
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Paragraph 0151; 0152, (2016/09/12)
The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I; and a method of treatment of a disorder or condition selected from the
Novel and high affinity fluorescent ligands for the serotonin transporter based on (S)-citalopram
Kumar, Vivek,Rahbek-Clemmensen, Troels,Billesb?lle, Christian B.,Jorgensen, Trine Nygaard,Gether, Ulrik,Newman, Amy Hauck
supporting information, p. 696 - 699 (2014/07/07)
Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently
Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3- dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites
Banala, Ashwini K.,Zhang, Peng,Plenge, Per,Cyriac, George,Kopajtic, Theresa,Katz, Jonathan L.,Loland, Claus Juul,Newman, Amy Hauck
, p. 9709 - 9724 (2014/01/06)
The serotonin transporter (SERT) is the primary target for antidepressant drugs. The existence of a high affinity primary orthosteric binding site (S1) and a low affinity secondary site (S2) has been described, and their relation to antidepressant pharmacology has been debated. Herein, structural modifications to the N, 4, 5, and 4′ positions of (±)citalopram (1) are reported. All of the analogues were SERT-selective and demonstrated that steric bulk was tolerated at the SERT S1 site, including two dimeric ligands (15 and 51). In addition, eight analogues were identified with similar potencies to S-1 for decreasing the dissociation of [3H]S-1 from the S1 site via allosteric modulation at S2. Both dimeric compounds had similar affinities for the SERT S1 site (Ki = 19.7 and 30.2 nM, respectively), whereas only the N-substituted analogue, 51, was as effective as S-1 in allosterically modulating the binding of [3H]S-1 via S2.
Method for the preparation of citalopram
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, (2008/06/13)
A method for the preparation of citalopram comprising reductive hydrolysis of a compound of Formula (IV) wherein R is a N,N-disubstituted amid group or an optionally substituted 4,5-dihydro-1,3-oxazol-2-yl group, and conversion of the resulting 5-formyl compound to citalopram.
