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,2,3 ). Without separation,  the mixture was directly coupled with the appropriate formic acid to give the target  compounds ( 4,5,6



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Abstracts ICPS 2023

1,2,3
). Without separation, 
the mixture was directly coupled with the appropriate formic acid to give the target 
compounds (
4,5,6
). The reaction were conducted in the presence of mixture two 
catalyzaters: 
N,N'
-dicyclohexylcarbodiimide (DCC) and
N,N
dimethylpyridin-4-amine 
(DMAP). The synthesis of new derivatives of 5-Fluorouracil have been continued. 
The structure of obtained derivates testified by: IR resolution Bruker Spectrum 
Invenio S-2021with ATR (4000 – 400 cm
-1
): 3321; 1571; 3072; 1713; 1079; 1342; 
2925; 1243; 1158; HPLC-Agilent Technologies 1260,(USA),column Poroshell 120 EC-
C18,2.7 µm,4,6 x100 мм detector-diode matrix detector; Redtime (5-FU-3.04); 3.23; 
2.90; 7.05. 
References:
1. Cunningham D; James, R. D. Integrating the oral fluoropyrimidines into the 
management of advanced colorectal cancer. 
Eur. J. Cancer 2001

37
, P.826-834.
2.Zhi-Yong Tian, Gang-Jun Du, Song-Qiang Xie, Jin Zhao, Wen-Yuan Gao, and Chao-
Jie Wang. Synthesis and Bioevaluation of 5-Fluorouracil derivatives

(in China). 
Molecules 2007,12, P. 2450-2457. 
3. Ozaki. S., Watanabe Y., Hoshiko T., Mizuno H., Ishikawa. K., Mori. H., 5-
Fluorouracil derivatives (IV): Synthesis of antitumor active acyloxyalkyl-5-fluouracils. 
Chem. Pharm. Bull. 
1984, 
32
, P.733-738. 


Poster presentation 
272 
SYNTHESIS OF DERIVATIVES OF LAGOXILIN WITH 
PHTHALIC ANHYDRIDE 
 
F.A. Sobirova, R.S. Esanov, A.D. Matchanov 
 
Institute of Bioorganic Chemistry named after acad. A.S. Sadykov 
Academy of Sciences of the Republic of Uzbekistan, Uzbekistan, Mirzo Ulugbek str., 
83, Tashkent, 100125 
 
A number of biologically active compounds have been isolated from the plant 
Lagochilus inebrians Bge
, a representative of the 
Lamiaceae
 
family, whose aqueous 
decoctions and tinctures are used for various bleeding, colds and allergies, and their 
physico-chemical parameters and spectral properties have been determined studied. The 
literature also shows that the main biologically active substance of the plant 
Lagochilus 
inebrians Bunge
is the diterpenoid lagochiline (3,16,17,18-tetrahydroxy-9,13-
epoxylabdan).
Today, it is important to look for anticoagulants and hemostatic agents among 1,4-
dicarboxylic acid derivatives, since the literature reports that carboxylic acid amides and 
hydrazides have hemostatic and anticoagulant effects. Amides and hydrazides of 
phthalic acid are obtained by certain methods from phthalic anhydride or 
tetrachlorophthalic acid. Dicarboxylic acids are also important in plant life. They have 
not only direct, but also secondary action. In particular, the immunobiological activity 
of terpenes promotes the activation of the phagocytosis process, and together with 
succinic acid improves the cellular and humoral control of neutrophils and 
macrophages. Based on these data, we set the task of carrying out the chemical 
synthesis of 3,16,17,18-tetrahydroxy-9,13-epoxylabdan (lagoсhilin), which is the main 
component of the plant 
Lagochilus inebrians Bunge
, with some representatives of a 
number of dicarboxylic acids, especially phthalic, glutaric and succinic anhydrides. The 
chemical synthesis of lagochilin with anhydrides of dicarboxylic acids was carried out 
in an absolute pyridine medium at the boiling point of pyridine. The course of the 
reaction was monitored by the TLC method. At the end of the reaction, pyridine was 
neutralized with a cold solution of hydrochloric acid. Some physico-chemical 
parameters of the synthesized substances have been studied. At the end of the reaction, 
pyridine was neutralized with a cold solution of hydrochloric acid. Some physico-
chemical parameters of the synthesized substances have been studied. Mono-, di-, tri-, 
tetra- , derivatives of lagochilin have a light yellow oily nature, insoluble in water. In 
our work, we took their sodium salts to ensure good solubility of esters in water. In 
addition, some physico-chemical parameters of the synthesized compounds were 
studied. in the IR - ν = (-C=O) 1750-1600; (C–O–C) 1450-1250, ν = (-ОН) 3500-3000; 
ν = (-СН
2,
–CH
3
)2900-2800. When analyzing the UV spectrum of the sodium 
salt of lagoxylin ester based on phthalic anhydride in the water:acetonitrile (1:1) system, 
an intense absorption maximum appears, corresponding to the n→p* transition in the 
UV spectrum of phthalic anhydride. at wavelengths of 238 and 293 nm. In the UV 
spectrum of the sodium salt of LgTF, a “hypsochromic” shift from 293 nm to 11 nm 
was observed; simultaneously with a “hypsochromic” shift by 6 nm, a “hyperchromic” 
effect was observed at an absorption maximum at 238 nm. 


Poster presentation 
273 

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