1010-26-0Relevant articles and documents
Preparation method of glutaryl imide derivative
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Paragraph 0037-0038; 0044-0045; 0051-0052, (2021/03/31)
The invention discloses a preparation method of a glutaryl imide derivative, which comprises the following steps: in a negative pressure state, dropwise adding acetic anhydride into molten 1, 1-cyclohexyl diacetic acid, and reacting to obtain 1, 1-cyclohexyl diacetic anhydride; adding ammonia water into an ammoniation kettle, dropwise adding 1, 1-cyclohexanediacetic anhydride to carry out ammoniation reaction, and adding hydrochloric acid to adjust the pH value, so as to obtain precipitated crystals, namely pentane valeric acid; adding pentane valeric acid, a toluene solvent and glacial aceticacid into the reaction kettle, heating, stirring, reacting, cooling, and carrying out suction filtration to obtain a filter cake; and adding the filter cake into ammonia water for soaking and stirring, carrying out suction filtration again, leaching with deionized water, and drying to obtain glutaryl imide. According to the preparation method of a glutaryl imide derivative, acetic anhydride and 1, 1-cyclohexyldiacetic acid are used as raw materials, so that the reaction efficiency is effectively improved, the product yield is increased, the production cost of the product is reduced, and producing benefits are improved.
VITRIFIED STATE STABILIZING AGENT FOR ANIMAL CELL CRYOPRESERVATION SOLUTION
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, (2018/06/29)
Provided are a vitrification stabilizer for animal cell cryopreservation fluid, and an animal cell cryopreservation fluid that exhibits superior vitrification capacity due to containing said vitrification stabilizer for animal cell cryopreservation fluid. The vitrification stabilizer for animal cell cryopreservation fluid contains an amphoteric polymer compound selected from the group consisting of: (a) an amphoteric polymer compound obtained by reacting ?-poly-L-lysine with butyl succinic acid anhydride and performing carboxylation; (b) an amphoteric polymer compound obtained by reacting ?-poly-L-lysine with butyl succinic acid anhydride and succinic acid anhydride, and performing carboxylation; and (c) an amphoteric polymer compound obtained by reacting ?-poly-L-lysine with a compound represented by formula (I) and performing carboxylation.
Synthesis of oxytocin analogues with replacement of sulfur by carbon gives potent antagonists with increased stability
Stymiest, Jake L.,Mitchell, Bryan F.,Wong, Susan,Vederas, John C.
, p. 7799 - 7809 (2007/10/03)
The neuropeptide oxytocin 1 controls mammary and uterine smooth muscle contraction. Atosiban 2, an oxytocin antagonist, is used for prevention of preterm labor and premature birth. However, the metabolic lifetimes of such peptide drugs are short because of in vivo degradation. Facile production of oxytocin analogues with varying ring sizes wherein sulfur is replaced by carbon (methylene or methine) could be achieved by standard solid-phase peptide synthesis using olefin-bearing amino acids followed by on-resin ring-closing metathesis (RCM). These were tested for agonistic and antagonistic uteronic activity using myometrial strips taken from nonpregnant female rats. Peptide 8 showed agonistic activity in vitro (EC50 = 1.4 × 103 ± 4.4 102 nM) as compared to 1 (EC50 = 7.0 ± 2.1 nM). Atosiban analogues 17 (pA2 = 7.8 ± 0.1) and 18 (pA2 = 8.0 ± 0.1) showed substantial activity compared to the parent oxytocin antagonist 2 (pA2 = 9.9 ± 0.3). Carba analogue 35 (pA2 = 6.1 ± 0.1) had an agonistic activity over 2 orders of magnitude less than its parent 3 (8.8 ± 0.5). A comparison of biological stabilities of 1,6-carba analogues of both an agonist 8 and antagonist 18 versus parent peptides 1 and 2 was conducted. The half-lives of peptides 8 and 18 in rat placental tissue were shown (Table 2) to be greatly improved versus their parents oxytocin 1 and atosiban 2, respectively. These results suggest that peptides 8 and 18 and analogues thereof may be important leads into the development of a long-lasting, commercially available therapeutic for initiation of parturition and treatment of preterm labor.
