Synthesis of sphingomyelin difluoromethylene analogue

As a new sphingomyelinase inhibitor, a novel sphingomyelin CF₂ analogue was designed and synthesized. One key step of this synthesis is the very mild hydrolysis of the oxazolidinone ring, a suitable intermediate for the introduction of a diethyl difluoromethylphosphonate group, by utilizing the characteristic electron withdrawing nature of the nosyl group at the oxazolidinone ring in an alcoholic solvent to produce the corresponding carbonate attaching at the secondary hydroxy group. The synthesized CF₂ analogue inactivated toward B. cereus sphingomyelinase with nearly the same attitude as the nitrogen analogue that we previously reported.     

Solution-phase synthesis of a muramyl dipeptide analogue MDA

The solution-phase synthesis of a muramyl dipeptide(MDP) analogue of N~α-[4-chlorocinnamoyl-L-alanyl-D-isoglutaminyl]-L-lysine (MDA,2) is reported that possesses the features of easy feasibility,safety and low cost in large scale of synthesis.     

A Click-Chemistry Linked 2′3′-cGAMP Analogue

2′3′-cGAMP is an uncanonical cyclic dinucleotide where one A and one G base are connected via a 3′-5′ and a unique 2′-5′ linkage. The molecule is produced by the cyclase cGAS in response to cytosolic DNA binding. cGAMP activates STING and hence one of the most powerful pathways of innate immunity. cGAMP analogues with uncharged linkages that feature better cellular penetrability are currently highly desired. Here, the synthesis of a cGAMP analogue with one amide and one triazole linkage is reported. The molecule is best prepared via a first Cu^I-catalyzed click reaction, which establishes the triazole, while the cyclization is achieved by macrolactamization.     

海南粗榧新碱类似物芳环的反常氢化反应（英文）

报道了海南粗榧新碱类似物芳环的一种反常氢化反应，并提出了可能的反应机理。     

A simple formula for an analogue of conditional wiener integrals and its applications II

Let C[0, T] denote the space of real-valued continuous functions on the interval [0, T] with an analogue w _ϕ of Wiener measure and for a partition 0 = t ₀ < t ₁ < ... < t _n < t _n+1 = T of [0, T], let X _n : C[0, T] → ℝ ⁿ⁺¹ and X ⁿ⁺¹: C[0, T] → ℝ ⁿ⁺² be given by X _n (x) = (x(t ₀), x(t ₁), ..., x(t _n )) and X _n+1(x) = (x(t ₀), x(t ₁), ..., x(t _n+1)), respectively. In this paper, using a simple formula for the conditional w _ϕ-integral of functions on C[0, T] with the conditioning function X _n+1, we derive a simple formula for the conditional w _ϕ-integral of the functions with the conditioning function X _n . As applications of the formula with the function X _n , we evaluate the conditional w _ϕ-integral of the functions of the form F _m (x) = ∫₀ ^T (x(t)) ^m for x ∈ C[0, T] and for any positive integer m. Moreover, with the conditioning X _n , we evaluate the conditional w _ϕ-integral of the functions in a Banach algebra which is an analogue of the Cameron and Storvick’s Banach algebra . Finally, we derive the conditional analytic Feynman w _ϕ-integrals of the functions in .      

新型含氟姜黄素类似物的合成、晶体结构及抗肿瘤活性

采用活性基团拼接法将含氟苯甲醛与酮反应, 合成了5个含氟单羰基姜黄素类似物, 结构经IR, ¹H NMR及ESI-MS确认. 对所合成的化合物进行了抗肿瘤活性测试(MTT法), 结果表明, 部分化合物对肿瘤细胞有较强的选择性抑制活性, 其中2,6-二(4-氟亚苯基)环己酮(3a)和2,6-二(2-氟亚苯基)环己酮(3b)的抗肿瘤谱广, 活性较好, 就此对化合物3b作了单晶培养, 并就晶体结构进行了X衍射分析. 结构表明化合物3b属三斜晶系, 空间群 P-1. 晶胞参数 a＝0.9222(2) nm, b＝0.9732(2) nm, c＝1.0127(2) nm, α＝88.920(4)°, β＝75.672(3)°, γ＝62.404(3)°, V＝0.7755(3) nm³, Z＝2, D_c＝1.329 Mg•m^－3, μ＝0.097 mm^－1, F(000)＝324, 最终偏离因子R＝0.0590, wR＝0.1841.     

A New Material Based on Nanostructured Prussian Blue Analogue Film Doped with Ce(III) for Development of Hydrogen Peroxide Sensor

Prussian blue analogue nanoparticles doped with Ce(III) (CeHCF) have been synthesized using chitosan (CS) and poly(diallyldimethylammonium chloride) (PDDA) as protective matrix and were cast onto a glassy carbon electrode surface directly. Transmission electron microscopy, UV‐Vis absorption spectroscopy and resonance Rayleigh scattering technique were employed to characterize the PB analogue nanoparticles protected with CS and PDDA. Compared with the bare glassy carbon electrode, the modified electrode exhibited excellent performances for determining H₂O_2. This work demonstrates the feasibility of the CS‐PDDA‐CeHCF nanoparticles modified glassy carbon electrode for practical sensing applications.     

SYNTHESIS OF ENDO-12-AMINOTRICYCLO[6.3.2.02,7]TRIDECA-2(7),3,5-TRIENE-12-EXO-CARBOXYLIC ACID: A NOVEL,CONFORMATIONALLY RESTRICTED PHENYLALANINE ANALOGUE

ABSTRACT

A seven step synthesis of the conformationally restricted phenylalanine analogue 9 from cycloheptadiene (1) is described.     

5－羟甲基－5－壬烷基戊内酯的合成

以已二酸为原料，经六步反应合成了５－羟甲基－５－壬烷基戊内酯，在形成手性中心的关键反应步骤中使用了（３Ｓ，４Ｓ）－１－苄基－１－甲基－３，４－二羟基吡咯碘化铵作手性相转移催化剂。