16179-41-2Relevant articles and documents
Voriconazole derivative, synthesis thereof, and use thereof in long-acting preparation
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Paragraph 0089, (2017/03/17)
The invention relates to a compound of formula (I), and a salt, an N-oxide, a quaternary ammonium and a stereoisomer thereof. R to R in the formula (I) are as defined in claims. The invention also relates to an intermediate for preparing the compound of formula (I), and a method for preparing the compound of formula (I). The invention further relates to a use of the compound of formula (I) as a drug especially used for preventing or treating fungal infection.
Posaconazole derivative, synthesis and application in prolonged action preparation thereof
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Paragraph 0087, (2017/04/03)
The invention relates to a posaconazole derivative, synthesis and an application in a prolonged action thereof. The invention relates to a formula of a compound and salt, N-oxide, quaternary ammonium and stereoisomer of the compound, wherein R1-R8 are defined according to what is claimed. The invention also relates to a preparation formula of an intermediate body and a method of the compound. The invention further relates to a formula of an application of the compound as a drug, especially the application in preventing or treating fungal infection. The detailed formulas are in the specification.
Combinatorial synthesis of PEG oligomer libraries
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Page/Page column 11, (2010/02/15)
A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.