Anri-effect

Anri-Markownikov hydration of alkenes may be effected indirectly by addition of B2H6 (hydroboratiori), followed by oxidation of the... 

Cyclobutenes are effective dienophiles.19-21 The stereochemistry of these reactions has been studied by employing 2,5-dimethyl-3,4-diphenylcyclopenta-2,4-dienone as the diene. Thus, r/.v-3,4-dich 1 orocyclobutene reacted with the dienone to give the anri,exo- and the anti,endo- so-mers 15 in a ratio of 4 1.22 Similar cycloaddition of the dienone with dimethyl tricy-clo[4,2,2.02 5]dcca-3,7,9-triene-7,8-dicarboxylatc gave the exo- and the rwfo-isomers 16 in a ratio of 6 1.22 The exo stereoselectivity is attributed to steric factors.22... 

The stage now set to effect the Sn2 reaction. [Fig. (27)] Compound 99 was refluxed in benzene with 20 equiv of NaH, resulting in a very clean and high-yielding cyclization reaction furnishing the desired product 100, and the undesired anri-diastereomer was not detected. 

Mercaptopurine [6-MP] (Purinettiol) [Anrineoplasric/ Anri metabolite] Uses Acute leukemias, 2nd-line Rx of CML NHL, maint ALL in children, immunosuppressant w/ autoimmune Dzs (Crohn Dz) Action Antimetabolite, mimics hypo xanthine Dose Adults. 80-100 mg/m2/d or 2.5-5 mg/kg/d maint 1.5-2.5 mg/kg/d Peds. Per protocol 4 w/ renal/hepatic insuff on empty stomach Caution [D, ] Contra Severe hepatic Dz, BM suppression, PRG Disp Tabs SE Mild hematotox, mucositis, stomatitis, D rash, fever, eosinophilia, jaundice, Hep Interactions T Effects Wl allopurinol T risk of BM suppression W/ trimethoprim-sulfamethoxazole 4 effects OF warfarin EMS May falsely T glucose OD May cause N/V and liver necrosis symptomatic and supportive Meropenem (Merrem) [Anribioric/Carbapenem] Uses Intra-abd Infxns, bacterial meningitis Action Carbapenem 4 cell wall synth, a 3-lac-tam Dose Adults. 1 to 2 g IV q8h Peds. >3 mo, <50 kg 10-40 mg/kg IV q 8h 4 in renal insuff Caution [B, ] Contra fl-Lactam sensitivity Disp Inj 500 mg, 1 g SE Less Sz potential than imipenem D, thrombocytopenia Interactions T Effects W/ probenecid EMS Monitor for signs of electrolyte disturbances and... 

Mesalamine (Asacol, Lialda, Pentasa, Rowasa) [Anri inflammatory/Salicylate] Uses Mild-mod distal ulcerative colitis, proctosigmoiditis, proctitis Action Unknown may inhibit prostaglandins Dose Rectal 60 mL qhs, retain 8 h (enema), 500 mg bid—tid or 1000 mg qhs (supp) PO Cap 1 g PO qid Tab 1.6-2.4 g/d - doses (tid—qid) delayed release 2.4—4.8 g PO daily 8 wk max, do not cut/crush/chew w/ food i initial dose in elderly Caution [B, M] Contra Salicylate sensitivity Disp Tabs, caps, supp, rectal susp SE HA, malaise, abd pain, flatulence, rash, pancreatitis, pericarditis Interactions 1 Effect OF digoxin EMS May turn urine yellow-brown OD May cause N/V/D, tinnitus, HA, and drowsiness activated charcoal may be effective... 

T effects OF amiodarone, astemizole, atorvastadn, barbiturates, bepridil, bupropion, cerivastatin, cisapride, clorazepate, clozapine, clarithromycin, desipramine, diazepam, encainide, ergot alkaloids, estazolam, flecainide, flurazepam, indinavir, ketoconazole, lovastatin, meperidine, midazolam, nelfinavir, phenytoin, pimozide, piroxicam, propafenone, propoxyphene, quinidine, rifabutin, saquinavir, sildenafil, simvastatin, SSRIs, TCAs, terfenadine, triazolam, troleandomycin, zolpidem X effects W/ barbiturates, carbamazepine, phenytoin, rifabutin, rifampin, St. John s wort, tobacco X effects OF didanosine, hypnotics, methadone, OCPs, sedatives, theophylline, warfarin EMS T Effects of amiodarone, diazepam, midazolam and BBs, may need X- doses concurrent use of Viagra-type drugs can lead to hypotension X- effects of warfarin concurrent EtOH use can T adverse effects T glucose ODs May cause an extension of adverse SEs symptomatic and supportive Rivasrigmine (Exelon) [Cholinesterase Inhibitor/Anri ... 

Homoallylic alcohols This combination generates a Sn(0) species, which is more effective than Sn-Al (12, 486) for diastereoselective reaction of cinnamyl chloride with aldehydes to form anri-homoallylic alcohols. 

Debromination. C24Fe effects stereospecific anri-debromination of wc-dibrom-ides(THF, 70°).1 It is an effective substitute for Fc2(CO)<,2 for generation of 2-oxyallyl cations from a,a -dibromo ketones (5, 222-223 6, 195-196 9,477-478). 

For bicyclopropyl each geometric species contains two torsion dependent C. .. C-distances. The positions of these distances are given in Fig. 10 both for anri and gauche. The effect of the large torsional amplitude in bicyclopropyl is demonstrated by the broad torsional dependent area in the RD-curve without well defined peaks. This is in contrast to the well defined nnri-peak in the corresponding part of the RD-curve for 1,3-butadiene. 

From these results, it appears that anri-deuterium substitution transmits its isotope effect better than gauc/ze-deuterium substitution, the same trend as is observed in transmission of coupling constants. 

In contrast to the case with 65a, the hydrogenation of dimethyl bicyclo[2.2.2]oct-2-ene-2,3-dicarboxylate (69) yields the syn-endo-addition product 70 over Rh-C and Pt-C in heptane at 25°C and 1 atmH2 (eq. 3.31).161,162 The hydrogenation over Pt-C, however, was accompanied by 7.1% of apparent anri-addition product 71. The presence of small amounts of a strong acid, which had little effect on the hydrogenation with rhodium, greatly increased the formation of 71 over Pd-C, which amounted to as much as 60% in the presence of p-TsOH in methanol. 

It was observed that an antf-homometa chloro group is selectively cleaved over that of an anri-homopara chloro group in the following bicyclic anisyl compound [74]. The meta effect in photochemistry was first demonstrated by Zimmerman... 

Gassman and Fentiman (1970) used the Brown equation to investigate participation by a remote ir-bond in solvolysis reactions. They compared substituent effects in the solvolyses of 7-aryl-7-norbornyl [6], and syn-l-aryl-anri-7-norbornenyl [7] systems. The saturated bicyclic system [6] gave a linear... 

In addition to the acetate aldol problem, stereoselective aldol additions of substituted enolates to yield 1,2-anti- or f/treo-selective adducts has remained as a persistent gap in asymmetric aldol methodology. A number of innovative solutions have been documented recently that provide ready access to such products. The different successful approaches to anri-selective propionate aldol adducts stem from the design of novel auxiliaries coupled to the study of metal and base effects on the reaction stereochemistry. The newest class of auxiliaries are derived from A-arylsulfonyl amides prepared from readily available optically active vicinal amino alcohols, such as cw-l-aminoindan-2-ol and norephedrine. 

Yamamoto found that, in general, the (Z)-stannanes 170 favored formation of the syn adducts 173 under thermal conditions, presumably through transition state 174 (Fig. 11-16). Under thermal conditions, however, the (F)-stannanes 171 generally favor formation of the anti adducts 172, where the anti stereochemistry is rationalized by reaction occurring through transition state 175. Also different from Keck s observations, Yamamoto found that the anri-adducts 172 were formed preferentially (via transition state 176) in the Lewis acid-promoted reactions of both the (Z)-170 and the ( )-171 substrates. Thus, as noted by Yamamoto, the secondary orbital interactions or the dipole effects experienced in the ring-closing transition states with the (y-alkoxyallyl)stannanes 170 and 171 are apparently not as important in the reactions of 158 and 159 [106]. 

Acceleration of aldol reactions.2 In the absence of a catalyst, silyl enol ethers ordinarily do not react with aldehydes even at high temperatures. Thus the dimcthylphenyl-silyl ether 2a does not react with C<,H jCHO at 150°. In contrast, the silacyclobutane analog (2b), prepared from 1, reacts with C HsCHO at 27° to form syn- and anri-aldols in 12 1 ratio. This stereoselectivity is the opposite of that obtained by the TiCI4-catalyzed reaction. l-Chloro-l-mcthylsilacyclobutane, CHi(CI)Si(CH2)3, is even more effective than 1 for this aldol reaction. It is prepared from (3-chloropropyl)dichloromethylsilane. It is particularly useful for aldol reactions with acyclic silyl ketene acetals (equation II). 

It is imperative to examine the effect of carcinogen-DNA adducts on the topology as well as conformation of DNA, since these properties are believed to influence the specific DNA interactions. From the spectroscopic studies (uv, CD, LD) it can be inferred that both B and Z forms of polynucleotides can covalently react with BaPDE with a very low affinity for the Z form [124, 127-128]. In fact, both diastereomers favour and preserve B-like conformations around the adduct site even at 4.5M NaCl. This might introduce flexibility in the poly (dG-dC). poly (dG-dC) structure manifested by a reduced LD signal [129]. Thus anri-BaPDE adduct formation may affect the behaviour of DNA selectively not only at the... 

Aldol reactions. Titanium -ate complexes effect anri-selective aldolization (5 examples, 72-81%). 

Budesonide, Oral (Entocorf EC) [Anri-inflammatory> CorHcosteroid] Uses Mild—mod Crohn Dz Action Steroid, anti-inflammatory Dose Adults. Initial, 9 mg PO qAM to 8 wk max maint 6 mg PO qAM taper by 3 mo avoid grapefruit juice Contra Active TB and fungal Infxn Caution [C, /-] DM, glaucoma, cataracts, HTN, CHF Disp Caps SE HA, cough, hoarseness, Candida Infxn, epistaxis Interactions T Effects W/ erytln omycin, indinavir, itraconazole, ketoconazole, ritonavir, grapefruit EMS Monitor ECG and BP for signs of electrolyte disturbances and hypovolemia OD Acute OD unlikely to cause a problem, clironic OD can reduce natural production of certain stei oids symptomatic and supportive... 

Nitrofurantoin (Macrodanrin, Furadanrin, Macrobid) [Urinary Anri-infective] WARNING Pulm Rxns possible Uses Prevendon Rx UTE Action Bacteriostatic iaterferes w/ carbohydrate metabolism. Dose Adults. Suppression 50-100 mg/d PO Rx 50-100 mg PO qid Peds. Suppression 1-2 mg/kg/d ia 1—2 + doses, max 100 mg/d Rx 5—7 mg/lcg/24 h ia 4 + doses (w/ food/milk/antacid) Caution [B, +] Avoid w/ CrCl <60 ml ymin, PRG at term Contra Renal failure, infants <1 mo Disp Cperipheral neuropathy Interactions T Effects W/ probenecid, sulfinpyrazone 4 effects w/ antacids, quinolones EMS May affect glucose (hypoglycemia) may discolor urine OD May cause N/V give IV fluids... 

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